Title of Invention	THIENO[2,3-D]-PYRIMIDINE-4(3H)-ONE COMPOUNDS AND PROCESS THEREOF
Abstract	The present invention discloses novel compounds of the Formula (1), containing thieno-[2,3-d]pyrimidin-4(3H)-one moieties and pharmaceutical ly acceptable salts thereof, methods for preparing these compounds, the use of these compounds in prevention and treatment of fungal infections, and pharmaceutical preparations containing these novel compounds.

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FORM 2 THE PATENT ACT 1970 (39 of 1970) & The Patents Rules, 2003 COMPLETE SPECIFICATION (See section 10 and rule 13) 1. TITLE OF THE INVENTION: "Thieno[2,3-d]-pyrimidine-4(3//)-one compounds with antifungal properties and process thereof 2. APPLICATION(S): A) (a) NAME: National Chemical Laboratory (b) NATIONALITY: Indian Research Centre (c) ADDRESS: Dr. Homi Bhabha Road, Pashan, Pune - 411 008, India B) (a) NAME: FDC Ltd. (b) NATIONALITY: Indian company incorporated under the Companies Act 1956 (c) ADDRESS: 142-48, S.V. Road, Jogeshwari (West), Mumbai - 400 102, Maharashtra, India. 3. PREAMBLE TO THE DESCRIPTION The following specification particularly describes the invention and the manner in which it is to be performed. Technical field The present invention relates to novel compounds of the Formula (1), containing thieno-[2,3-d]pyrimidin-4(3H)-ones moieties and pharmaceutically acceptable salts thereof, methods for preparing these compounds, the use of these compounds in prevention and treatment of fungal infections, and to pharmaceutical preparations containing these novel compounds. Background and prior art: Fungal infections are the major problem in the treatment of immuno- compromised patients and those suffering from AIDS. The current antifungal agents belong to various groups like polyenes, allylamines, antimetabolites, azoles, glucan synthesis inhibitors etc. Fluconazole is a member of the family of azole antifungals. Fluconazole is orally active and has low toxicity but its extensive use has resulted in emergence of fluconazole-resistant fungal strains. Therefore, it is necessary to meet the long-felt need to develop novel fluconazole analogues which exert high anti-fungal activity against various fungi including Candida albicans, Aspergillus niger and Fusarium proliferation with MIC values 2 to 8 fold lower than that of fluconazole. The presence of one triazole ring, halogenated phenyl ring and tertiary alcoholic oxygen functionality in fluconazole is necessary for activity. The present invention seeks to provide novel azoles and process thereof as an effort to come up with antifungal agents with broad spectrum of antifungal activity. Fluconazole analogues have been reported having antifungal activity in the literature. A series of fluconazole analogues incorporating azaindole and indole moieties were described in "Synthesis and anti-fungal activities of new fluconazole analogues with azoheterocycle moiety", Bioorg Med Chem Lett 2007 July 1; 17(13), 3686-9. Objects of the Invention: The primary objective of the present invention is to provide compounds of Formula (1), containing thieno-[2,3-d]pyrimidin-4(3H)-one moieties with high anti-fungal activity against various fungi including C. albicans, Aspergillus, niger and F. proliferatum and the process for the preparation of said antifungal compounds. Summary of the invention: Accordingly, to meet the above stated objective, the present invention discloses novel fluconazole analogues of Formula (1) containing thieno-[2,3-d]pyrimidin-4(3H)-one moieties, which are useful as antifungal compounds with MIC values 2 to 8 fold lower than that of fluconazole. In one aspect, the invention provides novel compounds of formula (1), wherein, Rl is hydrogen or halogen selected from fluorine, chlorine, bromine or iodine; R2 is hydrogen or halogen selected from fluorine, chlorine, bromine and iodine; and R3 and R4 which may be the same or different and each represents a hydrogen, alkyl group of linear or branched chain of 1 to 20 carbon atoms optionally substituted with aryl group, hydroxyl group, alkanoate group, acetoxy group, amino acetyloxy group, N-Boc-amino acetyloxy group, alkoxy(-OR) group (wherein R= alkyl group with 1 to 4 carbon atoms), benzyloxy, arylalkyl group (wherein the aryl group is phenyl which is either unsubstituted or substituted with alkyl group of 1 to 3 carbon atoms) or cycloalkyl group with 3 to 10 carbon atoms. R2 Formula 1 In another aspect, the invention provides a process for the preparation of the compounds of Formula (1) using various synthetic methods. Accordingly, the present invention describes a general process for the preparation of compounds of the Formula (1) wherein Rl, R2, R3 and R4 are as defined above, which comprises reacting substituted 2-aminothiophene-3- carboxylates of the Formula (3) with formamide and ammonium acetate to collect the thienopyrimidinones of the Formula (4), followed by reacting the compounds of the Formula (4) with epoxide of the Formula (5) in presence of a suitable base to obtain the compounds of the Formula 1. The said suitable base may be selected from various organic or inorganic bases well described in the art. In yet another aspect, the invention discloses a pharmaceutical preparation which comprises a compound of formula (1) in association with at least one pharmaceutical excipient. Detailed description: The invention will now be described in detail in connection with certain preferred and optional embodiments, so that various aspects thereof may be more fully understood and appreciated. According to the present invention, there are provided novel antifungal compounds of Formula (1). These compounds are analogues of fluconazole that are active against fungi and used in pharmaceutical preparations as active agents. In a preferred embodiment, there are provided the novel compounds of Formula 1, R2 Formula 1 wherein, Rl is hydrogen, halogen selected from fluorine, chlorine, bromine or iodine; R2 is hydrogen,, halogen selected from fluorine, chlorine, bromine or iodine, R3 and R4 which may the same or different and each represents a hydrogen, alkyl group of linear or branched chain of 1 to 20 carbon atoms optionally substituted with aryl group, hydroxyl group, alkanoate group, acetoxy group, amino acetyloxy group, N-Boc-amino acetyloxy group, alkoxy(-OR) group (wherein R= alkyl group with 1 to 4 carbon atoms), benzyloxy, arylalkyl group (wherein the aryl group is phenyl which is either unsubstituted or substituted with alkyl group of 1 to 3 carbon atoms) or cycloalkyl group with 3 to 10 carbon atoms. The present invention encompasses all the novel compounds and their stereochemically isomeric forms or their pharmaceutical ly acceptable salts. In another preferred embodiment, the invention describes process for preparation of the compounds of formula (1). The compounds of the present invention may be prepared by adapting the route depicted in Scheme 1. As depicted in Scheme 1, the compounds of Formula (3) are converted to the compounds of Formula (4), wherein R3 and R4 are as defined above. In a further step, the compounds of Formula (4) are converted to the compounds of Formula (1) by reacting with the compounds of Formula (5), wherein Rl is hydrogen or a halogen selected from fluorine, chlorine, bromine and iodine; R2 is hydrogen or a halogen selected from fluorine, chlorine, bromine and iodine. Scheme 1 - Accordingly, the general process for the preparation of compounds of Formula 1, comprises steps of: a) preparing 2-amino-4 and/or 5-substituted thiophene-3-carboxylate of formula (3), wherein Rl is methyl or ethyl; and R3 and R4 are as defined above by Gewald synthesis; b) contacting 2-amino-4 and/or 5-substituted thiophene-3-carboxylate of Formula (3) with formamide and ammonium acetate to obtain the thieno-[2,3-d]-pyrimidin- 4(3H)- . one of Formula (4), wherein R3 and R4 are as defined above, and c) treating the compound of Formula (4) with epoxide of Formula (5), wherein Rl and R2 are as defined above, in presence of a base to obtain the compound of Formula (1). The said suitable base may be selected from various organic or inorganic bases well described in the art. In another preferred embodiment, the invention discloses a pharmaceutical preparation which comprises a compound of formula (1) in association with at least one pharmaceutical excipient known in art. The invention further provides a method for treating or preventing a fungal infection in a subject, which comprises administering an effective amount of the compound of formula (1) in association with pharmaceutical excipients. The compounds of formula (1) can be conveniently administered to a patient in oral unit dosage form and prepared by any of the methods well-known in the pharmaceutical arts. Dosage forms include solid dosage forms like tablets, powders, capsules, sachets, troches and lozenges as well as liquid syrups, suspensions and elixirs. The active ingredient (s) and excipients can be formulated into compositions and dosage forms according to methods known in the art. Accordingly, the compounds of formula (1) or their pharmaceutically acceptable salt can be milled into a powder and be used in a pharmaceutical product/composition or physically modified such as by granulation to produce larger granules. The compounds of formula (1) or their pharmaceutical^ acceptable salt can also be used to prepare a liquid pharmaceutical composition by dissolving or dispersing or suspending/emulsifying it in a pharmaceutically acceptable liquid medium such as water, glycerin, vegetable oil and the like as discussed in greater detail below. When a dosage form such as a tablet is made by compaction of a powdered composition, the composition is subjected to pressure from a punch and dye. Solid and liquid compositions can also be dyed using any pharmaceutically acceptable colorant to improve their appearance and/or to facilitate patient identification of the product and unit dosage level. In liquid pharmaceutical compositions of the present invention, the compounds of formula (1) or their pharmaceutically acceptable salt and any other solid excipients are dissolved or suspended in a liquid carrier such as water, vegetable oil, alcohol, polyethylene glycol, propylene glycol or glycerin. Liquid pharmaceutical compositions can contain emulsifying agents to disperse an active ingredient or other excipient that is not soluble in the liquid carrier uniformly throughout the composition. Selection of particular excipients and the amounts to use can be readily determined by the formulation scientist based upon experience and consideration of standard procedures and reference works in the field. The solid compositions of the present invention include powders, granulates, aggregates and compacted compositions. The compounds of formula (1) or their pharmaceutical salt can also be used to prepare topical preparations such as shampoos, lotions, gels, foams, creams, transdermal patches and greasy ointments. Still in another object, the use of the compounds of formula (1) for the preparation of medicament useful for the treatment or prevention of fungal infections is provided by the invention. The invention is further illustrated with the following examples and should not be construed to limit the scope of the present invention. The features of the present invention will become more apparent from the following description of the inventive concept and the description of the preferred embodiments and appended claims. Example 1 General synthetic procedure for preparation of compounds of the Formula 1: Procedure A: Thienopyrimidinones of the Formula (4) (1 mmol), epoxide of formula (5) (1 mmol) and sodium methoxide (1.2 mmol) were taken in 2-neck RB flask under inert atmosphere, dry t-butanol (5-10 ml) was added to the above reaction mixture and the mixture was stirred under reflux for 10 to 30 hrs. Upon completion of the reaction, t-butanol was removed on rotavapor, water was added to the reaction mixture, the compound from the reaction mixture was extracted with ethyl acetate, dried and concentrated. Purification by column chromatography afforded the pure compounds of the Formula (1). Procedure B: Thienopyrimidinones of the Formula (4) (1 mmol) and epoxide of formula (5) (1 mmol) were taken in 2-neck RB flask under inert atmosphere, dry ethyl acetate (10-15 ml) was added followed by flame dried potassium carbonate (2 mmol) and tetrabutylammonium bromide (1.2 mmol). The mixture was stirred under reflux for 2 to 10 hrs, cooled, diluted with water, extracted with ethyl acetate, dried and concentrated. Purification by column chromatography afforded the pure compounds of the Formula (1). Some functional group transformations like debenzylation, deacetylation, protection of hydroxyl functionality etc provided more number of compounds. The following novel compounds of formula (1) were prepared by using the above synthetic methods (see Table 1). Example 2 6-(3-Benzyloxypropyl)-3-[2-(2,4-difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-ylpropyl]-thieno[2,3-d]pyrimidin-4(3H)-one (1-A02): 6-(3 -Benzyloxypropyl)- thieno[2,3-d]pyrimidin-4(3H)-one of Formula (4-A02) (3.0 g, O.Olmole), l[[2-(2,4-difluorophenyl)oxiranyl]methyl]-lH-l,2,4-triazole of the Formula (5) (2.82 g, 0.012 mole) and sodium methoxide (0.65 g, 0.012 mole), were taken in two neck round bottom flask under inert atmosphere, dry t-butanol (70 ml) was added to the above reaction mixture and the mixture was stirred under reflux for 12 hours. t-Butanol was removed on rotavapor, water (50 ml) was added to the reaction mixture, the compound from the reaction mixture was extracted with ethyl acetate (3 x 50 ml), dried, concentrated and purified by column chromatography to obtain the pure 6-(3-benzyloxypropyl)-3-[2-(2,4-difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-ylpropyl]-thieno[2,3-d]pyrimidin-4(3H)-one (1-A02) (0.8 gm, 14%).lHNMR (CDC13, 200 MHz): : 1.91-2.06 (m, 2H), 2.95 (t, J=6 Hz, 2H), 3.51 (t, J=6 Hz, 2H), 4.21 (d, J=14 Hz, 1H), 4.49 (s,2H),4.52(d,J=14Hz, 1H), 4.72 (d, J=14 Hz, 1H), 4.79 (d, J=14 Hz, lH),6.22(s, 1H), 6.72-6.88 (m, 2H), 7.08 (s, 1H), 7.31 (bs, 5H), 7.49-7.62 (m, 1H), 7.83 (s, 1H), 7.91 (s, 1H), 8.09 (s, 1H). Example 3 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-5,6,7,8-tetrahydrobenzothieno[2,3-d]pyrimidin-4(3H)-one (1-A09): 5,6,7,8-Tetrahydrobenzothieno[2,3-d]pyrimidin-4(3H)-one of Formula (4-A09) (1.0 g, 4.8 mmole), l[[2-(2,4-difluorophenyl)oxiranyl]methyl]-lH-l,2,4-triazole of the Formula (5) (1.38 g, 5.8 mmole) and sodium methoxide (0.31 g, 5.8 mmole), were taken in two neck round bottom flask under inert atmosphere, dry t-butanol (30 ml) was added to the above reaction mixture and the mixture was stirred under reflux for 12 hours. t-Butanol was removed on rotavapor, water (20 ml) was added to the reaction mixture, the compound from the reaction mixture was extracted with ethyl acetate (3 x 20 ml), dried, concentrated and purified by column chromatography to obtain the pure 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-5,6,7,8- tetrahydrobenzothieno[2,3-d]pyrimidin-4(3H)-one (1-A09) (1.29 gm, 60%). lHNMR (CDC13, 200 MHz): 1.74-1.96 (m, 4H), 2.71-2.81 (m, 2H), 2.90-3.02 (m, 2H), 4.18 (d, J=14 Hz, 1H), 4.55 (d, J=14 Hz, 1H), 4.70 (d, J=14 Hz, 1H), 4.77 (d, J=14 Hz, 1H), 6.29 (bs, 1H), 6.72-6.92 (m, 2H),7.51-7.62 (m, 1H), 7.85 (s, 2H), 8.13 (s, 1H). Example 4 3- [2-(2,4-Difluorophenyl)-2-hydroxy-3- [ 1,2,4] triazol- 1-y 1-propy 1] -6-(3- acetoxypropyl)-thieno[2,3-d]pyrimidin-4(3H)-one (1-A26): 6-(3-Acetoxypropyl)- thieno[2,3-d]pyrimidin-4(3H)-one of Formula (4-A26) (0.5 g, 2 mmole) and l[[2-(2,4-difluorophenyl)oxiranyl]methyl]-lH-l,2,4-triazole of the Formula (5) (0.47 g, 2 mmole) were taken in two neck round bottom flask under inert atmosphere, dry ethyl acetate (5 ml) was added followed by flame dried potassium carbonate (0.55 g, 4 mmole) and tetrabutylammonium bromide (0.76 g, 2.4 mmole) the mixture was stirred under reflux for 12 hours, Cooled, diluted with water (15 ml) , extracted with ethyl acetate (3x10 ml), dried, concentrated and purified by column chromatography afforded the pure 3-[2-(2,4-difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-(3-acetoxypropyl)-thieno[2,3-d]pyrimidin-4(3H)-one (1-A26 ) (0.3 gm, 31%). lHNMR (CDC13, 200 MHz): 1.96-2.10 (m, 2H), 2.06 (s, 3H), 2.92 (t, J=8 Hz, 2H), 4.11 (t, J=6 Hz, 2H), 4.27 (d, J=14 Hz, 1H), 4.60 (d, J=14 Hz, 1H), 4.73 (d, J=14 Hz, 1H), 4.85 (d, J=14 Hz, 1H), 6.74-6.92 (m, 2H), 7.10 (s, 1H), 7.45-7.59 (m, 1H), 7.91 (bs, 1H), 7.95 (s, 1H), 8.36 (bs, 1H). Following compounds were prepared by following either of the general procedures described above. 5) 6-(4-Benzyloxybutyl)-3-[2-(2,4-difluorophenyI)-2-hydroxy-3-[l,2,4]triazol-l- ylpropyl]-thieno[2,3-d]pyrimidin-4(3H)-one (1-A01): This compound was prepared by procedure B using 6-(4-benzyloxybutyl)- thieno[2,3-d]pyrimidin-4(3H)-one and 1[[2- (2,4-difluorophenyl)oxiranyl]methyl]- lH-l,2,4-triazole of the Formula (5). lHNMR (CDC13, 200 MHz): 1.61-1.86 (m, 4H), 2.84 (t, J=6 Hz, 2H), 3.49 (t, J=6 Hz, 2H), 4.23 (d, J=16 Hz, 1H), 4.49 (s, 2H), 4.53 (d, J= 16 Hz, 1H), 4.72 (d, J=16 Hz, 1H), 4.80 (d, J=16 Hz, 1H), 6.22 (s, 1H), 6.72-6.90 (m, 2H), 7.08 (s, 1H), 7.32 (bs, 5H), 7.50-7.62 (m, 1H), 7.84 (s, 1H), 7.92 (s, 1H), 8.10 (s, 1H). 6) 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-(n-hexyl)- thieno[2,3-d]pyrimidin-4(3H)-one (1-A03): lHNMR (CDC13, 200 MHz): : 0.88 (t, J=6 Hz, 3H), 1.21-1.48 (m, 6H), 1.61-1.76 (m, 2H), 2.82 (t, J=8 Hz, 2H), 4.22 (d, J=15 Hz, 1H), 4.52 (d, J=15 Hz, 1H), 4.72 (d, J=15 Hz, 1H), 4.80 (d, J=15 Hz, 1H), 6.24 (s, 1H), 6.75-6.89 (m, 2H), 7.07 (s, 1H), 7.48-7.62 (m, 1H), 7.83 (s, 1H), 7.91 (s, 1H), 8.10 (s, 1H). 7) 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-n-pentylthieno[2,3-d]pyrimidin-4(3H)-one (1-A04): lHNMR (CDC13, 200 MHz): : 0.90 (t, J=6 Hz,3H), 1.27-1.42 (m, 4H), 1.64-1.76 (m, 2H), 2.82 (t, J=8 Hz, 2H), 4.21 (d, J=15 Hz, 1H), 4.52(d, J=15 Hz, 1H), 4.71 (d, J=15 Hz, 1H), 4.78 (d, J=15 Hz, 1H), 6.24 (s, 1H), 6.76-6.88 (m,2H), 7.06 (s, 1H), 7.50-7.64 (m, 1H), 7.81 (s, 1H), 7.90 (s, 1H), 8.09 (s, 1H). 8) 5-n-Butyl-3-[2-(2,4-difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-n-propyl-thieno[2,3-d]pyrimidin-4(3H)-one (1-A05): lHNMR (CDC13, 200 MHz): : 0.93 (t, J=6 Hz, 3H), 0.99 (t, J=6 Hz, 3H), 1.30-1.48 (m, 2H), 1.58-1.76 (m, 4H), 2.73 (t, J=6 Hz, 2H), 2.78-2.96 (m, 2H), 4.29 (d, J=14 Hz, 1H), 4.59 (d, J=14 Hz, 1H), 4.64 (d, J=14 Hz, 1H), 4.76 (d, J=14 Hz, 1H), 6.40 (bs, 1H), 6.72-6.89 (m, 2H), 7.48-7.60 (m, 1H), 7.86 (s, 2H), 8.18 (s,lH). 9) 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-n-heptylthieno[2,3-d]pyrimidin-4(3H)-one (1-A06):lHNMR (CDC13, 200 MHz): : 0.86 (t, J=6 Hz,3H), 1.21-1.32 (m, 8H), 1.62-1.72 (m, 2H), 2.81 (t, J=8 Hz, 2H), 4.23 (d, J=15 Hz, 1H), 4.53(d, J=15 Hz, 1H), 4.72 (d, J=15 Hz, 1H), 4.80 (d, J=15 Hz, 1H), 6.24 (bs, 1H), 6.74-6.89 (m,2H), 7.06 (s, 1H), 7.48-7.60 (m, 1H), 7.84 (s, 1H), 7.91 (s, 1H), 8.13 (s, 1H). 10) 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-3,5,6,7-tetrahydrocyclopenta[4,5]thieno[2,3-d]pyrimidin-4(3H)-one (1-A07): lHNMR (CDC13, 200 MHz): 2.39-2.55 (m, 2H), 2.95 (t, J=7 Hz, 2H), 3.02 (t, J=7 Hz, 2H), 4.18 (d, J=14 Hz, IH), 4.55 (d, J=14 Hz, IH), 4.73 (d, J=14 Hz, IH), 4.80 (d, J=14 Hz, IH), 6.26 (bs, IH), 6.74-6.92 (m, 2H), 7.51-7.63 (m, IH), 7.85 (s, 2H), 8.15(s, IH). 11) 3-[2-(2,4-Difluorophenyl)- 2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]- 6-methyl- 5-npentyl-thieno[2,3-d]pyrimidin-4(3H)-one (1-A08): lHNMR (CDC13, 200 MHz): : 0.89 (t, J=6 Hz, 3H), 1.22-1.50 (m, 6H), 2.39 (s, 3H), 2.71-2.93 (m, 2H), 4.27 (d, J=14 Hz, IH), 4.58- 4.81 (m, 6H), 6.41 (bs, IH), 6.72-6.88 (m, 2H), 7.48-7.62 (m, IH), 7.85 (bs, 2H), 8.18 (bs, IH). 12) 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-n-hexyl-5- methyl-thieno[2,3-d]pyrimidin-4(3H)-one (1-A10): LHNMR (CDC13, 200 MHz): : 0.88 (t, J=6 Hz, 3H), 1.20-1.43 (m, 6H), 1.55-1.68 (m, 2H), 2.44 (s, 3H), 2.74 (t, J=8Hz, 2H), 3.20 (bs,lH), 4.22 (d, J=14 Hz, IH), 4.59-4.88 (m, 6H), 6.74-6.92 (m, 2H), 7.48-7.62 (m, IH), 7.89 (bs,2H), 8.39 (bs, IH). 13) 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yI-propyl]-5-methyl-6-npentyl-thieno[2,3-d]pyrimidin-4(3H)-one (1-A11): LHNMR (CDC13, 200 MHz): : 0.90 (bt, J=6 Hz, 3H), 1.30-1.45 (m, 4H), 1.56-1.69 (m, 2H), 2.43 (s, 3H), 2.74 (t, J=8Hz, 2H), 4.24 (d, J=14 Hz, IH), 4.66 (d, J=14 Hz, IH), 4.74 (d, J=14 Hz, IH), 4.86 (d, J=14 Hz, IH), 6.72-6.92(m, 2H), 7.46-7.59 (m, IH), 7.92 (s, IH), 7.95 (s, IH), 8.55 (bs, IH). 14) 6-(7-Acetoxyheptyl)-3-[2-(2,4-difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-ylpropyl]-thieno[2,3-d]pyrimidin-4(3H)-one (1-A12):LHNMR (CDC13, 200 MHz): : 1.21- 1.36 (m, 6H), 1.51-1.80 (m, 4H), 2.03 (s, 3H), 2.81 (t, J=8 Hz, 2H), 4.03 (t, J=6 Hz, 2H), 4.25 (d, J=14 Hz, IH), 4.56 (d, J=14 Hz, IH), 4.72 (d, J=14 Hz, IH), 4.82 (d, J=14 Hz, IH), 6.72- 6.88 (m, 2H), 7.06 (s, IH), 7.47-7.61 (m, IH), 7.87 (bs, IH), 7.92 (s, IH), 8.23 (bs, IH). 15) 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-(7- hydroxy heptyl)-thieno[2,3-d]pyrimidin-4(3H)-one (1-A13): 6-(7-Acetoxyheptyl)-3-[2-(2,4-difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-ylpropyl]-thieno[2,3-d]pyrimidin-4(3H)-one (3.00 g, 5.5 mmol) was dissolved in the mixture of methanol (10 ml) and water (2 ml). Then potassium carbonate (760 mg, 5.5 mmol) was added and the mixture was stirred at RT for 2 hours. Methanol was then removed on rotavapor, water (10 ml) was added to the reaction mixture and extracted with ethyl acetate (2x5 ml), dried, concentrated and purified by column chromatography to obtain the pure 3-[2-(2,4-difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-(7-hydroxyheptyl)-thieno[2,3-d]pyrimidin-4(3H)-one (2.5 gm, 90.57%). lHNMR (CDC13, 200 MHz): 1.25-1.42 (m, 6H), 1.49-1.80 (m, 4H), 2.81 (t, J=8 Hz, 2H), 3.62 (t, J=6 Hz, 2H), 4.25 (d, J=14 Hz,lH), 4.57 (d, J=14 Hz, IH), 4.72 (d, J=14 Hz, IH), 4.82 (d, J=14 Hz, IH), 6.27 (bs, IH), 6.72-6.89 (m, 2H), 7.06 (s, IH), 7.42-7.61 (m, IH), 7.87 (bs, IH), 7.92 (s, IH), 8.25 (bs, IH). 16) 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-5(2- phenylethyl)-thieno[2,3-d]pyrimidin-4(3H)-one (1-A14): 1HNMR (CDC13, 200 MHz): 2.90 (t, J=8 Hz, 3H), 3.22 (t, J=8 Hz, 3H), 4.30 (d, J=14 Hz, IH), 4.63 (d, J=14 Hz, IH), 4.72 (d, J=14 Hz, IH), 4.86 (d, J=14 Hz, IH), 6.70-6.90 (m, 3H), 7.15-7.31 (m, 5H), 7.40-7.61 (m, IH), 7.90 (bs, IH), 7.99 (s, IH), 8.33 (bs, IH). 17) 6-Benzyl-3-[2-(2,4-difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-5- methyl-thieno[2,3-d]pyrimidin-4(3H)-one (1-A15): 1HNMR (CDC13, 200 MHz): : 2.51 (s, 3H), 4.09 (s, 2H), 4.21 (d, J=14 Hz, IH), 4.61 (d, J=14 Hz, IH), 4.74 (d, J=14 Hz, IH), 4.84 (d, J=14 Hz, IH), 6.65-6.91 (m, 2H), 7.15-7.34 (m, 5H), 7.45-7.61 (m, IH), 7.89 (s, IH), 7.90 (s, IH), 8.36 (bs, IH). 18) 6-n-Decyl-3-[2-(2,4-difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]- thieno [2,3-d] pyrimidin-4(3H)-one (1-A16): LHNMR (CDC13, 200 MHz): : 0.87 (t, J=6 Hz, 3H), 1.14-1.44 (m, 14H), 1.55-1.77 (m, 2H), 2.81 (t, J=8 Hz, 2H), 4.27 (d, J=14 Hz, IH), 4.61 (d, J=14 Hz, IH), 4.72 (d, J=14 Hz, IH), 4.84 (d, J=14 Hz, IH), 6.73-6.92 (m, 2H), 7.06 (s, IH), 7.44-7.61 (m, IH), 7.90 (bs, IH), 7.93 (s, IH), 8.35 (bs, IH). 19) 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]- 6-n-nonylthieno[2,3-d] pyrimidin-4(3H)-one (1-A17): LHNMR (CDC13, 200 MHz): : 0.86 (t, J=6H, 3H), 1.13-1.42 (m, 12H), 1.54-1.80 (m, 2H), 2.80 (t, J=8 Hz, 2H), 4.26 (d, J=14 Hz, 1H),4.57 (d, J=14 Hz, IH), 4.72 (d, J=14 Hz, IH), 4.82 (d, J=14 Hz, IH), 6.27 (bs, IH), 6.73-6.92(m, 2H), 7.06 (s, IH), 7.44-7.61 (m, IH), 7.87 (bs, IH), 7.92 (s, IH), 8.25 (bs, IH). 20) 3- [2-(2,4-Difluoropheny l)-2-hydroxy-3- [ 1,2,4] triazol-1 -y I-propyl]-6-(n-propyl)- thieno[2,3-d]pyrimidin-4(3H)-one (1-A18): LHNMR (CDC13, 200 MHz): : 0.99 (t, J=7 Hz, 3H), 1.61-1.83 (m, 2H), 2.80 (t, J=8 Hz, 2H), 4.27 (d, J=14 Hz, IH), 4.59 (d, J=14Hz, IH), 4.73 (d, J=14 Hz, IH), 4.84 (d, J=14Hz, IH), 6.28 (bs, IH), 6.74-6.90 (m, 2H), 7.08 (s, IH), 7.46-7.61 (m, IH), 7.88 (s, IH), 7.92 (s, IH), 8.28 (s, IH). 21) 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]- 3,5,6,7,8,9,10,11,12,13,14-undecahydrocyclododeca[4,5]thieno[2,3-d]pyrimidin- 4(3H> one (1-A19): lHNMR (CDC13, 200 MHz): : 1.10-1.57 (m, 12H), 1.59-1.83 (m, 4H), 2.66-2.97(m, 4H), 4.27 (d, J=14 Hz, IH), 4.58 (d, J=14Hz, IH), 4.66 (d, J=14 Hz, IH), 4.79 (d, J=14Hz, IH), 6.33 (bs, IH), 6.72-6.90 (m, 2H), ^,46-7.90 (m, IH), 7.86 (s, IH), 7.89 (s, IH), 8.20 (s, IH). 22) 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazoI-l-yl-propyl]- 5-methyl- 6-n-octyl-thieno[2,3-d]pyrimidin-4(3H)-one (1-A20):lHNMR (CDC13, 200 MHz): : 0.91 (t, J=6 Hz, 3H), 1.18-1.49 (m, 10H), 1.56-1.75 (m, 2H), 2.48(s, 3H), 2.78 (t, J-8Hz, 2H), 4.22 (d, J=14 Hz, IH), 4.59 (d, J=14 Hz, IH), 4.77 (d, J=14 Hz, IH), 4.84 (d, J=14 Hz, IH), 6.31 (bs,lH), 6.80-6.92 (m, 2H), 7.54-7.72 (m, IH), 7.90 (bs, 2H), 8.20 (bs, IH). 23) 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-n-butyl-5- methyI-thieno[2,3-d]pyrimidin-4(3H)-one (1-A21): lHNMR (CDC13, 200 MHz): : 0.93 (t, J=6 Hz, 3H), 1.28-1.45 (m, 2H), 1.52-1.69 (m, 2H), 2.43 (s, 3H), 2.74 (t, J=8Hz, 2H), 4.20 (d, J=14 Hz, IH), 4.60 (d, J=14 Hz, IH), 4.74 (d, J=14 Hz, IH), 4.84 (d, J=14 Hz, IH), 6.72- 6.90 (m, 2H), 7.48-7.59 (m, IH), 7.88 (bs, 2H), 8.34 (bs, IH). 24) 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6- ethylthieno [2,3-d]pyrimidin-4(3H)-one (1-A22): 1HNMR (CDC13, 200 MHz): : 1.35 (t, J=7 Hz, 3H), 2.87 (q, J=7 Hz, 2H), 4.27 (d, J=14 Hz, IH), 4.60 (d, J=14Hz, IH), 4.72 (d, J=14 Hz, IH), 4.83 (d, J=14Hz, IH), 6.26 (bs, IH), 6.77-6.91 (m, 2H), 7.08 (s, IH), 7.48-7.61 (m, IH), 7.89 (s, 1H), 7.92 (s, 1H), 8.31 (s, 1H). 25) 3- [2-(2,4-Difluoropheny l)-2-hydroxy-3- [ 1,2,4] triazol-1 -yl-propyl] -6-(4- hydroxybutyl)-thieno[2,3-d]pyrimidin-4(3H)-one (1-A23): lHNMR (CDC13, 200 MHz): : 1.50-1.90 (m, 4H), 2.87 (t, J=6 Hz, 2H), 3.59 (t, J=6 Hz, 2H), 4.26 (d, J= 14 Hz, 1H), 4.56 (d, J=14 Hz, 1H), 4.77 (d, J=14 Hz, 1H), 4.89 (d, J=14 Hz, 1H), 6.22 (bs, 1H), 6.72-6.92 (m, 2H), 7.07 (s, 1H), 7.35-7.50 (m, 1H), 7.76 (bs, 1H), 8.00 (s, 1H), 8.22 (bs, 1H). 26) 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-(4-N-BocaminoacetyIoxybutyl)-thieno[2,3-d]pyrimidin-4(3H)-one (1-A24): A mixture of -[2-(2,4-difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-(4-hydroxybutyl)-thieno[2,3-d]pyrimidin-4(3H)-one (500 mg, 0.895 mmol), Boc-glycine (188 mg, 1.073 mmol), DMAP (10 mg) in DCM (10 ml) was taken at 0°C and added EDCI (257 mg, 1.34 mmol) to it and stirred for 2 hours. It was then diluted with water (10 ml), extracted with DCM (2x5 ml), dried, concentrated and purified by column chromatography to obtain the pure 3-[2-(2,4-difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-(4-N-Bocaminoacetyloxybutyl)-thieno[2,3-d]pyrimidin-4(3H)-one (300 mg, 46.87%). lHNMR (CDC13, 200MHz): : 1.47 (s, 9H), 1.62-1.90 (m, 4H), 2.80-2.96 (m, 2H), 3.78-3.98 (m, 2H), 4.05-4.32 (m,3H), 4.55-4.91 (m, 3H), 5.05 (bs, 1H), 6.29 (bs, 1H), 6.73-6.89 (m, 2H), 7.12 (s, 1H), 7.50-7.65 (m, 1H), 7.92 (bs, 1H), 7.98(s, 1H), 8.35 (bs, 1H). 27)3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yI-propyl]-6-(4-aminoacetyloxybutyl)-thieno[2,3-d]pyrimidin-4(3H)-one (1-A25): 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-(4-N-Bocaminoacetyloxybutyl)-thieno[2,3-d]pyrimidin-4(3H)-one (200 mg, 0.28 mmol) was dissolved in DCM (6 ml) at 0°C. Trifluoroacetic acid (0.129 ml, 191 mg, 1.68 mmol) was added to it and stirred for 4 hours. It was then diluted with water (10 ml), extracted with DCM (2x5 ml), dried, concentrated and purified by column chromatography to obtain the pure 3-[2-(2,4-difluorophenyl)-2-hydroxy-3-[ 1,2,4]triazol-1 -yl-propyl]-6-(4-aminoacetyloxy butyl)-thieno[2,3-d]pyrimidin-4(3H)-one (100 mg, 56.81%). lHNMR (CDC13, 200 MHz): 1.45-1.80 (m, 4H), 2.68-2.90 (m, 2H), 4.05-4.29 (m, 4H), 4.32-4.61 (m, 3H), 4.65-4.90 (m, 3H), 5.81 (bs, 1H), 6.68-6.91 (m, 2H), 7.03 (s, 1H), 7.39-7.58 (m, 1H), 7.74 (s, 1H), 7.91 (s, 1H), 8.08 (s, 1H). 28) 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-(3-hydroxypropyl)-thieno[2,3-d]pyrimidin-4(3H)-one (1-A27): LHNMR (CDC13 + DMSOd6,200 MHz): 1.68-1.84 (m, 2H), 2.77 (t, J=8 Hz, 2H), 3.47 (t, J=6 Hz, 2H), 4.12 (d, J=14 Hz, IH), 4.47 (d, J=14 Hz, IH), 4.61 (d, J=14 Hz, IH), 4.83 (d, J=14 Hz, IH), 6.54-6.76 (m,2H), 6.93 (s, IH), 7.12-7.35 (m, 3H), 7.86 (s, IH). 29) 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6- methylthieno[2,3-d]pyrimidin-4(3H)-one (1-A28): LHNMR (CDC13, 200 MHz): : 2.51 (s, 3H),4.23 (d, J=12 Hz, IH), 4.53 (d, J=12Hz, IH), 4.69 (d, J=12 Hz, IH), 4.77 (d, J=12 Hz, 1H),6.22 (bs, IH), 6.70-6.85 (m, 2H), 7.04 (s, IH), 7.45-7.60 (m, IH), 7.83 (s, IH), 7.90 (s, lH),8.10(s, IH). The pharmaceutical salts of the compounds of Formula (1) can be prepared by known methods and obvious modifications. Table 1: Analogues of fluconazole of Formula (1) Compo und No. R1 R2 R^ R' Sample >'o. 1 2-F 4-F CH3 H 1-A28 •j 2-Cl 4-C1 CH3 H 3 2-Br 4-Br CH3 H 4 2-F H CH3 H 5 2-C1 H CH 3 H 6 2-Br H CH3 H : H 4-F CH3 H 8 H 4-C1 CH 5 H 9 H 4-Br CH3 H 10 2-F 4-F H CH3 11 2-C1 4-C1 H CH3 12 2-Br 4-Br H CH 3 13 2-F H H CH3 14 2-C1 H H CH3 15 2-Br H H CH3 16 K 4-F H CH 3 17 H 4-C1 H CH3 18 H 4-Br H CH3 19 2-F 4-F CH2CH3 H 1-A22 20 2-C1 4-C1 CH2CH3 H 21 2-Br 4-Br CH2CH3 H ■>'"> 2-F H CH2CH3 H 2} 2-C1 H CH2CH3 H 24 2-Br H C'H2CH3 H 25 H 4-F CH2CH3 H 26 H 4-Cl CH2CH3 H 27 H 4-Br CH2CH3 H 28 2-F 4-F H CH2CH3 29 2-C1 4-C1 H CH2CH3 30 2-Br 4-Br H CH2CH3 31 2-F H H CH2CH3 32 2-C1 H H CH2CH3 33 2-Br H H CH2CH3 34 H 4-F H CH2CH3 35 H 4-C1 H CH2CH3 36 H 4-Br H CH2CH3 37 2-F 4-F (CH2)2CH3 H 1-A18 38 2-C1 4-C1 (CH2)2CH3 H 39 2-Br 4-Br (CH2)2CH3 H 40 2-F H (CH2)2CH3 H 41 2-C1 H (CH2)2CH3 H 42 2-Br H (CH2)2CH3 H 43 K 4-F (CH2)2CH3 H 44 H 4-C1 (CH2)2CH3 H 45 H 4-Br (CH2)2CH3 H 46 2-F 4-F H (CH2)2CH3 47 2-C1 4-C1 H (CH2)2CH3 48 2-Br 4-Br H (CH2)2CH3 49 2-F H H (CH2)2CH3 50 2-C1 H H (CH2)2CH3 5! 2-Br H H (CH2)2CH3 52 H 4-F H (CH2)2CH3 53 H 4-C1 H (CH2)2CH3 54 H 4-Br H (CH2)2CH3 55 2-F 4-F (CH2)3CH3 H 56 2-C1 4-C1 (CH2)3CH3 H 57 2-Br 4-Br (CH2)3CH3 H 58 2-F H (CH2)3CH3 H 59 2-C1 H (CH2)3CH3 H 60 2-Br H (CH2)2CH3 H 19 61 H 4-F (CH:)3CHj H 62 H 4-C1 (CH2)JCHJ H 63 H 4-Br (CH2)3CH3 H 64 2-F 4-F H (CH2)3CH3 65 2-C1 4-Cl H (CH2)3CH3 66 2-Br 4-Br H (CH2)3CH3 67 2-F H H (CH2)3CH3 68 2-C1 H H (CH2)3CH3 69 2-Br H H (CH2):,CH3 70 H 4-F H (CH2)3CH3 71 H 4-C1 H (CH2)3CH3 -j-i H 4-Br H (CH2)3CH3 73 2-F 4-F (CH,)4CH3 H 1-A04 74 2-Cl 4-C1 (CH^CH;, H 75 2-Br 4-Br {CH2)XH3 H 76 2-F H (CH2)4CH3 H 77 2-Cl H (CH2)4CH3 H 78 2-Br H (CH:),CH3 H 79 H 4-F (CH2),CH3 H 80 H 4-C1 (CH2KH3 H 81 H 4-Br (CH2)*CH3 H 82 2-F 4-F H (CH;)4CH3 S3 2-Cl 4-C1 H (CH2j4CH3 84 2-Br 4-Br H (CH2)4CH3 85 2-F H H (CH2)4CH3 86 2-Cl H H (CH2)4CH5 87 2-Br H H (CH2)4CH3 88 H 4-F H (CH2)4CH3 89 H 4-C1 H (CH2)4CH3 90 H 4-Br H (CH2)4CH3 91 2-F 4-F (CH>)sCHi H 1-A03 92 2-Cl 4-C1 (CH2)5CH3 H 20 93 2-Br 4-Br (CH2)5CH3 H 94 2-F H (CH2)5CH3 H 95 2-C1 H (CH2)SCH3 H 96 2-Br H 97 H 4-F ICH2)5CH3 H 98 H 4-C1 (CH2)SCH3 H 99 H 4-Br {CH:)5CH5 H 100 2-F 4-F H (CH2)SCH3 101 2-C1 4-C1 H [CH2)5CH3 102 2-Br 4-Br H (CH2)5CH3 103 2-F H H (CH2)5CH3 104 2-C1 H H (CH2)5CH3 105 2-Br H H (CH2)?CH3 106 H 4-F H (CH2')5CH3 107 H 4-C1 H (CH2)5CH3 108 H 4-Br H (CH2)5CH3 109 2-F 4-F (CH2)6CH, H 1-A06 110 2-C1 4-C1 (CH2)«CH3 H 111 2-Br 4-Br (CH;)JCHJ H 112 2-F H (CH2)6CH3 H 113 2-C1 H (CH2)«CH3 H 114 2-Br H (CH:)«CHj H 115 H 4-F (CH2)«CH3 H 116 H 4-C1 (CH2)«CH3 H 117 H 4-Br (CH2)«CH3 H 118 2-F 4-F H (CH2)*CH3 119 2-C1 4-C1 H (CH2)SCH3 120 2-Br 4-Br H (CH2)jCH3 121 2-F H H (CH2)SCH3 122 2-C1 H H (CH2)«CH3 123 2-Br H H (CH2)«CH3 U4 H 4-F H (CH2)«CH3 21 125 H 4-C1 H (CH2)SCH3 126 H 4-Br H (CH2)«C:H3- 127 2-F 4-F (CH2)7CH3 H 12S 2-C1 4-C1 129 2-Br 4-Br (CH2)7CH3 H 130 2-F H (CH2)7CH3 H 131 2-C1 H (CH2)7CH3 H 132 2-Br H {CH2)7CH3 H 133 H 4-F (CH2)7CHj H 134 H 4-C1 (CH2)7CH3 H 135 H 4-Br (CH2)7CH3 H 136 2-F 4-F H (CH2)7CH3 137 2-C1 4-C1 H (CH2)-CH3 13S 2-Br 4-Br H (CH2)7CHJ 139 2-F H H iCH2)-CH3 140 2-C1 H H (CH2)7CH3 141 2-Bf H H (CH2)7CH3 142 H 4-F H (CH2)-CH3 143 H 4-C1 H (CH2) 144 H 4-Br H (CH2)7CH3 145 2-F 4-F {CHihCHj H 1-A17 146 2-CI 4-C1 (CHsKHs H 147 2-Br 4-Br fCH2)3CH3 H 148 2-F H (CH2)aCH3 H 149 2-CI H (CH2)SCH3 H 150 2-Br H (CH2)8CH3 H 151 H 4-F (CH2)jCH3 H 152 H 4-C1 (CH2)3CH3 H 153 H 4-Br (CH2)3CHS H 154 2-F 4-F H (CH2)gCH3 155 2-C1 4-C1 H (CH2)sCH3 156 2-Bf 4-Br H (CH2)8CH3 22 157 2-F H H (CH2)»CH3 158 2-C'l H H (CH2)BCH3 159 2-Br H H (CH2)gCH3 160 H 4-F H (CH2)»CH3 161 H 4-Cl H (C'H2)sCHj 162 H 4-Br H (CH2)gCH3 163 2-F 4-F (CHjfeCH, H 1-A16 164 2-C1 4-C1 fCH2)9CH3 H 165 2-Br 4-Br (CH2)9CH3 H 166 2-F H (CH2)9CH3 H 167 2-C1 H {CH2)9CHj H 168 2-Br H (CH2)9CH3 H 169 H 4-F (CH2)9CH3 H 170 H 4-C1 (CH2>CH5 H 171 H 4-Br (CH:>pCH3 H 172 2-F 4-F H (CH2)5CH3 173 2-C1 4-Cl H (CH2)«CH3 174 2-Br 4-Br H (CH2)9CH3 175 2-F H H (CH2)9CH3 176 2-C1 H H (C H2)gCH3 177 2-Br H H (C H2)5CH3 17S H 4-F H (CH2)9CHJ 179 H 4-Cl H (CH2)QCH3 180 H 4-Br H (CH2)?CH3 181 2-F 4-F CHj CHj 182 2-C1 4-Cl CH;, CH3 183 2-Br 4-Br C'H5 CH3 184 2-F H CH3 CH3 185 2-C1 H CHj CH3 186 2-Br H CHj CH3 187 H 4-F CHj CH3 188 H 4-Cl CH3 CH3 23 189 H 4-Br CH3 CH3 190 2-F 4-F CH3 CH2CH3 191 2-Cl 4-CI CH3 CH3CH3 192 2-Br 4-Br CH3 CH2CH3 193 2-F H CH3 CH2CH3 194 2-C1 H CH3 CH2CH3 195 2-Br H CH3 CH2CH3 196 H 4-F CH3 CH2CH3 197 H 4-Ci CH3 CH3CH3 198 H 4-Br CH3 CH2CH3 199 2-F 4-F CH3 (CHO,CH3 200 2-C1 4-CI CH3 (CH2):CH3 201 2-Br 4-Br CH3 (CH2)2CH3 202 2-F H CH3 (CH2):CH3 203 2-C1 H CH3 (CH2)2CH3 204 2-Br H CH3 (CH2)2CH3 205 H 4-F CH3 (C'H2)2CH3 206 H 4-CI C'H3 (CH2)2CH3 207 H 4-Br CH3 (CH2)2CH3 20S 2-F 4-F CH3 (CH2)3CH3 209 2-C1 4-CI CH3 (CH2)3CH3 210 2-Br 4-Br CH3 (CH2)3CH3 211 2-F H CH3 (CH2)3CH3 212 2-C1 H CH3 (CH2)3CH3 213 2-Br H CH3 (CH2)3CH3 214 H 4-F CH3 (CH2)3CH3 215 H 4-CI CH3 (CH2)3CH3 216 H 4-Br CH3 (CH2)3CH3 217 2-F 4-F CH| (CH2)4CHi 1-A08 21S 2-C1 4-CI CH3 (CH2)4CH3 219 2-Br 4-Br CH3 (CH2)4CH3 220 2-F H CH3 ICH2;I4CH3 VM 221 2-Cl H CH3 (CH2)4CHj -VT> 2-Br H CHj (CH2)4CH5 223 H 4-F CHj (CH2)4CHj 224 H 4-C1 CHj (CH;)4CHJ 225 H 4-Br CHj (CH2)4CHJ 226 2-F 4-F CHj (CH2)5CH3 ■> i"? 2-Cl 4-C1 CHj (CH;)SCHJ 228 2-Br 4-Br CHj (CH;)SCHJ 229 2-F H CHj (CH2)SCHJ 230 2-Cl H CHj (CH2)SCHJ 231 2-Br H CHj (CH2)5CH3 232 H 4-F CHJ (CH2)5CHJ 233 H 4-C1 CHJ (CH2)5CH3 234 H 4-Br CHJ (CH2)5CHJ 235 2-F 4-F CHJ (CH2)JCHJ 236 2-Cl 4-C1 CHJ (CH2IJCHJ 237 2-Br 4-Br CHJ (CH2)5CHJ 238 2-F H CHJ (CH2)5CHJ 239 2-Cl H CHJ (CH2)SCHJ 240 2-Br H CHJ (CH2)«CH3 241 H 4-F CHJ (CH2)5CHJ 242 H 4-C1 CHJ (CH2)sCHj 243 H 4-Br CHJ (CH2)*CHj 244 2-F 4-F CHJ (CH2)TCHJ 245 2-Cl 4-C1 CHJ (CH2hCHj 246 2-Br 4-Br CHJ (CH2)7CH3 247 2-F H CHJ (CH2;hCHj 248 2-Cl H CHJ (CH2)-CHj 249 2-Br H CHJ (CH2)-CHj 250 H 4-F CHJ (CH2)7CH3 251 H 4-C1 CHJ (CH2)7CHj 252 H 4-Br CHJ (CH2KHj 2£T 253 2-F 4-F CH3 (CH2)gCH3 254 2-C1 4-C1 CHJ (CH2)gCH3 255 2-Br 4-Br CHj (CH2),CHj 256 2-F H CHj (CH2JsCHj 257 2-C1 H CH3 (CH2)gCHs 25S 2-Br H CH3 (CH2)gCH3 259 H 4-F CHj (CH2)gCH3 260 H 4-C1 CH5 (CH2)BCH3 261 H 4-Br CHj (CH2)gCH3 262 2-F 4-F CH2CH3 CH3 263 2-C1 4-C1 CH2CH5 CH3 264 2-Br 4-Br CH2CH3 CH3 265 2-F H CH2CH3 CH3 266 2-C1 H CH2CH3 CH3 267 2-Br H CH2CH3 CH3 26S H 4-F CH2CH3 CH3 269 H 4-C1 CH2CH3 CH3 270 H 4-Br CH2CH3 CH3 271 2-F 4-F (CH2)2CH3 CH3 272 2-C1 4-C1 (CH2)2CH3 CH3 273 2-Br 4-Br (CH2)2CH3 CH3 274 2-F H (CH2)2CH3 CHJ 275 2-Cl H (CH2)2CHj CH3 276 2-Br H (CH2)2CH3 CH3 277 H 4-F (CH2)2CH3 CH3 27S K 4-C1 (CH2)2CH3 CHj 279 H 4-Br (CH2)2CH3 CHJ 280 2-F 4-F (CH2)SCH3 CHJ 281 2-C1 4-Cl (CH2)3CH3 CH3 282 2-Br 4-Br (CH2)jCH3 CH3 283 2-F H (CH2)3CH3 CHj 284 2-C1 H (CH2)jCH3 CHJ 26 2S5 2-Br H lCH2)3CH3 CHJ 286 H 4-F lCH2)3CH3 CH3 287 H 4-C1 (CH2)3CH3 CH3 288 H 4-Br (CH2)3CH3 CH3 289 2-F 4-F (CH2)iCHj CHj 1-A11 290 2-C1 4-C1 (CH2)4CH3 CH3 291 2-Br 4-Br CCH2)XH3 CHj 292 2-F H (CH&CHs CH3 293 2-C1 H (CHO4CH3 CH3 294 2-Br H (CH2)4CHj CH3 295 H 4-F (CH2KH3 CH3 296 H 4-C1 (CH:)JCHS CH3 297 H 4-Br (CH2)4CHJ CH3 298 2-F 4-F (CH2)5CHj CHj 1-A10 299 2-C1 4-C1 (CH2)5CH3 CH3 300 2-Br 4-Br (CH2)5CH3 CH3 301 2-F H (CH2)sCH3 CH3 302 2-C1 H (CH2)5CH3 CH3 303 2-Br H (CH2).5CH3 CHj 304 H 4-F (CH2)sCH3 CHJ 305 H 4-C1 {CH2)5CH3 CH3 306 H 4-Br (CH2)jCH3 CHj 307 2-F 4-F (CH2)«CH3 CHJ 308 2-C1 4-C1 (CH2)«CH3 CH3 309 2-Br 4-Br (CH:)«CH3 CH3 310 2-F H (CH2)«CH3 CH3 311 2-C1 H (CH2)aCH3 CH3 312 2-Br H (CH2)«CH3 CHj 313 H 4-F lCH2)ijCH3 CHJ 314 H 4-C1 (CH2)«CH3 CHj 315 H 4-Br (CH2)«CH3 CH3 316 2-F 4-F (CH2)7CH3 CHj 27 317 2-C1 4-Cl (CH2)7CH3 CH3 318 2-Br 4-Br (CH2)7CH3 CH3 319 2-F H (CH2)7CH3 CH5 320 2-C1 H (CH2)7CH3 CH3 321 2-Br H (CH2KH3 CH3 322 K 4-F (CH2)7CH3 CH3 323 K 4-C1 (CH2)7CH3 CH3 324 H 4-Br (CH2)7CH3 CH3 325 2-F 4-F (CH;)sCH3 CH3 326 2-C1 4-C1 (CH2)SCH3 CH3 32.7 2-Br 4-Br (CH2)8CH3 CH3 328 2-F H (CH2)8CH3 CH3 329 2-C1 H (CH2)8CH3 CH3 330 2-Br H (CH2)8CH3 CH3 331 H 4-F (CH2)3CH3 CH3 332 H 4-Cl (C H2j8C H3 CH3 333 H 4-Br (CH2)8CH3 CH3 334 2-F 4-F - 335 2-C1 4-Cl -(CH2)3- = RJ 336 2-Br 4-Br -(CH2)j- = R> 337 2-F H -{CH2)3- = RJ 338 2-Cl H -(CH:)3- = R"' 339 2-Br H -{CH2)3- = R* 340 H 4-F -(CH2)3- = R* 341 H 4-Cl ■(CH2)j- = R: 342 H 4-Br -{CH2)3- = R' 343 2-F 4-F - 344 2-Cl 4-Cl -(CH2)«- = RJ 345 2-Br 4-Br - 346 2-F H -1CH2)4- = R' 347 2-Cl H -(CH2)4- = R' 348 2-Br H -(CH2),- = Rj 28 349 H 4-F -(CH2)*- = R'" 350 H 4-C1 -(CH;),- = K! 351 H 4-Br -(CH2),- = RJ 352 2-F 4-F -CCH2)5- = RJ 353 2-Cl 4-C1 - 354 2-Br 4-Br -(CH;)5- = RJ 355 2-F H -(CH2)5- = R> 356 2-Cl H -(CH2)5- = R* 357 2-Br H -(CH2)5- = RJ 358 H 4-F -(CH2)s- = R' 359 H 4-C1 -(CH2)5- = Rj 360 H 4-Br -(CH2)5- = R"' 361 2-F 4-F -{CH2)r = R* 362 2-C1 4-C1 -(CH2)«- = Rj 363 2-Br 4-Br -(CH2)«- = R' 364 2-F H •{CH2)«- = RJ 365 2-C1 H -{CH2)r = RJ 366 2-Br H -(CH2)6- = R' 367 H 4-F -(CH2)a- = RJ 368 H 4-C1 -(CH2V = R> 369 H 4-Br -(CH2)«- = K3 370 2-F 4-F -{CH2)7- = R- 371 2-C1 4-Cl -(CH2>- = RJ 372 2-Br 4-Br -(CH2)7- = R* 373 2-F H -(CH:)v = R" 374 2-C1 H -(CH2>- = R5 375 2-Br H -{CH2)7- = RJ 376 H 4-F -(CH2>- = R* 377 H 4-C'l -(CH2)7- = R3 37S H 4-Br -(CH:)7- = RJ 379 2-F 4-F -(C'H2)S- = RJ 380 2-Cl 4-Ci -CCH2)3- = Ri 2 381 2-Br 4-Br -(CH2)S- = R' 382 2-F H -(CH2)3- = RJ 383 2-C1 H -(CH;)3- = RJ 3 84 2-Br H -(CH;)S- = R3 385 H 4-F -(CHiV = R3 386 H 4-C1 -(CH;)s- = R3 387 H 4-Br -lCH;)S- = RJ 388 2-F 4-F -(CH2)9- = Ki 389 2-C1 4-C1 -(CH2)9- = BJ 390 2-Br 4-Br -ccH2y = R' 391 2-F H -(CH2)9- = R3 392 2-C1 H -(CH2)9- = RJ 393 2-Br H -ICH2)9- = RJ 394 H 4-F -tCH2)o- = R' 395 H 4-C1 -{CH2)9- = R' 396 H 4-Br -(CH2)9- = R* 39? 2-F 4-F -(CH2)1C- = R3 398 2-C1 4-C1 -(CH2)10- = RJ 399 2-Br 4-Br -(CH2)io- = R* 400 2-F H -tCH2)]0- = R 401 2-C1 H -(C'H2)]o- = R> 402 2-Br H -{CH2)]c- = R' 403 H 4-F -(CH2)]0- = R' 404 H 4-C1 -(CH2)io- = RJ 405 H 4-Bi - 406 2-F 4-F CH2OH H 407 2-C1 4-C1 CH2OH H 40S 2-Br 4-Br CH2OH H 409 2-F H CH2OH H 410 2-C1 H CH2OH H 411 2-Br H CH2OH H 412 H 4-F CH2OH H 3o 413 H 4-C1 CH2OH H 414 H 4-Br CH;OH H 415 2-F 4-F CH2CH2OH H 416 2-C1 4-C1 CH2CH2OH H 417 2-Br 4-Br CH2CH2OH H 41S 2-F H CH2CH2OH H 419 2-C1 H CH2CH2OH H 420 2-Br H CH2CH2OH H 421 H 4-F CH2CH2OH H 422 H 4-Ci CH2CH2OH H 423 H 4-Br CH2CH2OH H 424 2-F 4-F (CH2>,CH2OH H 1-A 27 425 2-C1 4-C1 (CH2)2CH2OH H 426 2-Br 4-Br (CH2)2CH2OH H 427 2-F H l'CH2);CH20H H 428 2-C1 H (CH2)2CH2OH H 429 2-Br H (CH2)2CH2OH H 430 H 4-F (CH2)2CH2OH H 431 H 4-C1 (CH2)2CH2OH H 432 H 4-Br (CH2)2CH2OH H 433 2-F 4-F (CH2),CHjOH H 1-A 23 434 2-C1 4-Ci (CH2)3CH2OH H 435 2-Br 4-Br (CH2)3CH2OH H 436 2-F H (CH2)3CH2OH H 437 2-C1 H (CH2)5CH2OH H 438 2-Br H (CH2)3CH2OH H 439 H 4-F (C'H2)5CH2OH H 440 H 4-CI (CH2)3CH2OH H 441 H 4-Br (CH:)3CH2OH H 442 2-F 4-F (CH2)4CH2OH H 443 2-C1 4-CI (CHJ^CHJOH H 444 2-Br 4-Br (CH2)4CH2OH H 3/ 445 2-F H (CH2)4CH2OH H 446 2-C1 H (CH2)*CH2OH H 447 2-Br H (CH2)*CH2OH H 448 H 4-F (CH2)4CH2OH H 449 H 4-Cl (CH2),CH2OH H 450 H 4-Br (CH2)*CH2OH H 451 2-F 4-F (CH2)5CH2OH H 452 2-C1 4-Cl (CH2)sCH2OH H 453 2-Br 4-Br (CH2)sCH2OH H 454 2-F H (CH2)5CH2OH H 455 2-C1 H (CH2)5CH2OH H 456 2-Bf H (CH2)iCH2OH H 457 H 4-F (CH2)5CH2OH H 458 H 4-Cl (CH2)sCH2OH H 459 H 4-Br (CH2)5CH2OH H 460 2-F 4-F (CH2)(CH2OH H 1-A13 461 2-C1 4-Cl (CH2)«CH2OH H 462 2-Br 4-Br (CH2)«CH2OH H 463 2-F H (CH2)«CH2OH H 464 2-C1 H (CH2)«CH2OH H 465 2-Br H {CH2) 466 H 4-F fCH2)«CH2OH H 467 H 4-Cl (CH2)«CH2OH H 46S H 4-Br (CH2)«CH2OH H 469 2-F 4-F (CH2)7CH2OH H 470 2-Cl 4-Cl (CH2)7CH2OH H 471 2-Br 4-Br (CH2)7CH2OH H AT-i 2-F H (CH2)7CH2OH H 473 2-Cl H (CH2)?CH2OH H 474 2-Bf H (CH2) 475 H 4-F (CH2)7CH2OH H 476 H 4-Cl tCH2)?CH2OH H 21 477 H 4-Br (CH2KH2OH H 47S 2-F 4-F (CH2)aCH2OAc H 479 2-C1 4-C1 (CH2)aCH2OAc H 480 2-Br 4-Br (CH2)aCH2OAc H 481 2-F H (CH2)aCH2OAc H 482 2-C1 H (CH2)aCH2OAc H 483 2-Br H (CH2)aCH2OAc H 484 H 4-F (CH2)aCH2OAc H 485 H 4-C1 (CH2)aCH2OAc H 486 H 4-Br (CH2)aCH2OAc H 487 2-F 4-F (CH2)2CH,OAc H 1-A26 4SS 2-C1 4-C1 (CH2)2C'H2OAc H 489 2-Bi 4-Br (CH2)2CH2OAc H 490 2-F H (CH2)2CH2OAc H 491 2-C1 H (CH2)2CH2OAc H 492 2-Br H (CH2)2CH2GAc H 493 H 4-F (CH2)2CH2OAc H 494 H 4-C1 (CH2)2CH2OAc H 495 H 4-Br (CH2)2CH2OAc H 496 2-F 4-F (CH2)sCHjOAc H 1-A12 497 2-C1 4-C1 (CH2)«CH2OAc H 498 2-Br 4-Br (CH2)«CH2OAc H 499 2-F H (CH2)«CH2OAc H 500 2-C1 H (CH2)«CH2OAc H 501 2-Br H (CH2)«CH2OAc H 502 H 4-F (CH2)*CH2OAc H 503 H 4-C1 (CH2)«CH2OAc H 504 H 4-Br (CH2)«CH2OAc H 505 2-F 4-F (CH2)aCH2OCOR H 506 2-C1 4-C1 tCH2)aCH2OCOR H 507 2-Br 4-Br (CH2)aCH2OCOR H 508 2-F H (CH2)aCH2OCOR H 33 509 2-C1 H (CH2)aCH2OCOR H 510 2-B.t H (CH2)ftCH2OCOR H 511 H 4-F (CH2)aCH2OCOR H 512 H 4-Cl (CH2)aCH2OCOR H 513 H 4-Br (CH2)aCH2OCOR H 514 2-F 4-F (CH2)aCH2OR H 515 2-C1 4-Cl (CH2)aCH2OR H 516 2-Br 4-Br (CH2)aCH2OR H 517 2-F H (CH2)aCH2OR H 518 2-C1 H (CH2)aCH2OR H 519 2-Br H (CH2)aCH2OR H 520 H 4-F (CH2)aCH2OR H 521 H 4-Cl (CH2)aCH2OR H 522 H 4-Br (CH2)aCH2OR H 523 2-F 4-F CCHjhCHiOBn H 1-A02 524 2-C1 4-Cl (CH2)2CH2OBn H 525 2-Br 4-Br (CH2)2CH2OBn H 526 2-F H (CH2)2CH2OBn H 527 2-C1 H (CH2)2CH2OBn H 52S 2-Br H (CH2)2CH2OBn H 529 H 4-F (CH2)2CH2OBn H 530 H 4-Cl (CH2)2CH2OBu H 531 H 4-Br (CH2)2CH2OBn H 532 2-F 4-F (CH3)iCH2OBn H 1-A01 533 2-C1 4-Cl (CH2);,CH2OBii H 534 2-Br 4-Br (CH2)3CH2OBn H 535 2-F H (CH2)3CH2OBu H 536 2-C1 H (CH2)5CH2OBn H 537 2-Br H (CH2)iCH2OBu H 538 H 4-F (CH2)jCH2OBn H 539 H 4-Cl (CH2)3CH2OBn H 540 H 4-Br (CH2)5CH2OBn H 3*f 541 2-F 4-F (CH&CHjR H 542 2-Cl 4-C1 (CH2)aCH2R H 543 2-Bi 4-Br (CH2)aCH2R H 544 2-F H (CH2)aCH2R H 545 2-C1 H (CH2)aCH2R H 546 2-Br H (CH2)aCH2R H 547 H 4-F (CH2)aCH2R H 548 H 4-Cl (CH2)aCH2R H 549 H 4-Br (CH2)aCH2R H 550 2-F 4-F CH2Ph (CH^CH^R 551 2-Cl 4-C1 CH2Ph (CH2)UCH2R 552 2-Br 4-Br CH2Ph (CH2)aCH2R 553 2-F H CH2Ph (CH2)ECH2R 554 2-Cl H CH2Ph (CH2)»CH2R 555 2-Br H CH2Ph (CH2)aCH2R 556 K 4-F CH2Ph (CH2)11CH2R 557 H 4-C1 CH2Ph (CH2)ECH2R 55S H 4-Br CH2Ph (C'H2)aCH2R 559 2-F 4-F CH2Ph CH3 1-A15 560 2-C1 4-C1 CH2Ph CH3 561 2-Br 4-Br CH2Ph CH3 562 2-F H CH2Ph CH3 563 2-C1 H CH2Ph CHj 564 2-Br H CH2Ph CH3 565 H 4-F CH2Ph CH3 566 H 4-C1 CH2Ph CH3 567 H 4-Br CH2Ph CH3 56S 2-F 4-F H (CH2kCH2Pli 569 2-C1 4-C1 H (CH2)nCH2Ph 570 2-Br 4-Br H (CH2iaCH2Ph 571 2-F H H (CH2)nCH2Ph 572 2-C1 H H (C'H2)aCH2Ph 35" 573 2-Br H H (CH2)nCH2Ph 574 H 4-F H (CH2)sCH2Ph 575 H 4-C1 H (C'H2)BCH2Pli 576 K 4-Br H (CH2)aCH2Ph 577 2-F 4-F H CHiCHiPh 1-A14 578 2-C1 4-C1 H CH2CH2Ph 579 2-Br 4-Br H CH:CH2Ph 580 2-F H H CH2CH2Ph 581 2-C1 H H CH2CH2Ph 582 2-Br H H CH2CH2Ph 5S3 K 4-F H CH2CH2Ph 584 H 4-C1 H CH2CH2Ph 585 H 4-Br H CH2CH2Ph 586 2-F 4-F C€H2)aCH20€OCH2NHBoe H 587 2-C1 4-C1 CCH2)aCH2QCOCH:NHBoc H 5SS 2-Br 4-Br (CH2)aCH2OCOCH;NHBoc H 589 2-F H (CH2)aCH2OCOCH:NHBoc H 590 2-C1 H (CH2)aCH2OCOCH:NHBoc H 591 2-Br H (CH2)aCH2OCOCH:NHBoc H 592 H 4-F (C'H2)aC'H2OC:OC'H2NHBoc H 593 H 4-C1 (CH2)aCH2QCOCH:NHBoc H 594 H 4-Br (CH2)aCH2OCOCH2NHBoc H 595 2-F 4-F (CH2)iCH2OCOCH2XHBoc H 1-A24 596 2-C1 4-C1 {CH2)3C'H2OC OCH2NHBoc H 597 2-Br 4-Br (CH2);XH2OCOCH2NHBoc H 598 2-F H (CH2)jCH2OCOCH;NHBoc H 599 2-C1 H (CH2)5CH2OCOCH:NHB oc H 600 2-Br H (CH2)iCH2OCOCH:NHBoc H 601 H 4-F CCH2)3CH2OCOCH2NHBoc H 602 H 4-C1 (CH2)3CH2OCOCH:NHBoc H 603 H 4-Br (CH2)jCH2OCOCH2NHBoc H 604 2-F 4-F CCH2)aCH2OCOCH2NHR H 36 605 2-Cl 4-C1 CCH2)aCH2OCQCH:NHR H 606 2-Br 4-Br (CH2)aCH2OCOCH:NHR H 607 2-F H (CH2)aCH2OCGCH2NHR H 60S 2-C1 H (CH^CHsOCOCHiNHR H 609 2-Br H (CH2)3CH2OCOCH;NHR H 610 H 4-F (CH2)aC H2OCOCH;NHR H 611 H 4-C1 (CH2)a.CH2OCOC'H:NHR H 612 H 4-Br (CH2)aCH2OCOCH:NHR H 613 2-F 4-F (CH2)iCH2OCOCHzNH2 H 1-A25 614 2-C1 4-C1 (CH2)3CH2OCOCH;NH: H 615 2-Br 4-Br (CH2)3CH2OCOCH;NH2 H 616 2-F H (CH2)3CH2OCOCH:NH2 H 617 2-C1 H (CH2)jCH2OCOCH;NH; H 618 2-Br H CCH2)3CH2OCGCH2NH2 H 619 H 4-F (CH2)3CH2OCOCH:NH: H 620 H 4-C1 (CH2)3CH2OCOCH;NH2 H 621 H 4-Br (CH2)3CH2OCOCH:NH2 H 622 2-F 4-F (CH2)aC'Hj (CH2)aCH3 623 2-C1 4-C1 (CH2)aCH3 (CH2)ftCH3 624 2-Br 4-Br (CH2)aCH3 (CH2)ttCH3 625 2-F H (CH2)aC'Hj (CH2)ttC:H3 626 2-C1 H (CH:)aCHi (CH2)aCHj 627 2-Br H (CH2)aC'Hj (CH2)BCH3 62S H 4-F (CH2)BCH3 (CH^CHj 629 H 4-C1 (CH2)aC-H3 (CHs^CHj 630 H 4-Br (C-H2)aCH3 (CHACHj 631 2-F 4-F (CH2)2CH3 (CH2)3CH3 1-A05 632 2-C1 4-C1 (CH2)2CHj (CH2)3CH3 633 2-Br 4-Br (CH2)2CH3 (CH2)3CH3 634 2-F H (CH2)2CHj (CH2)3CH3 635 2-C1 H (CH2)2CH3 (CH2)3CH3 636 2-Br H (CH2)2CH3 (CH2)3CH3 37 637 H 4-F (CH:);CH5 (CH;)3CHj 638 H 4-C1 (CH2)2CH3 (CH2)3CH3 639 H 4-Br (CH2)2CH3 (CH2)3CH3 Example 5 General method of preparation of compounds of Formula 4: A mixture of compound of Formula (3) (lmmol), ammonium acetate (1-10 mmol) and formamide (10-20 mmol) was stirred under reflux for 2 to 20 hrs, cooled, diluted with water, extracted with ethyl acetate, dried, concentrated and purified by column chromatography to obtain the compound of the Formula (4). The following compounds were prepared by the method described above: 1) 6-(4-Benzyloxypropyl)- thieno[2,3-d]pyrimidin-4(3H)-one (4-A02): A mixture of ethyl 2-amino-5-(3-benzyloxypropyl)-thiophene-3-carboxylate of Formula (3-A02): (5.5 g, 0.017 mole), ammonium acetate (10.6 g, 0. 14 mole) and formamide (17.12 ml, 0.43 mole), was stirred under reflux at 145°C for 12 hours. It was then cooled, diluted with water (50 ml), extracted with ethyl acetate (3 x 30 ml), dried, concentrated and purified by column chromatography to obtain the pure 6-(4-Benzyloxypropyl)-thieno[2,3-d]pyrimidin-4(3H)-one of Formula (4-A02) (4.5 gm, 87.2%). 1HNMR (CDC13, 200 MHz): 1.91-2.12 (m, 2H), 3.01 (t, J=6 Hz, 2H), 3.53 (t, J=6 Hz, 2H), 4.51 (s, 2H), 7.17 (s, 1H), 7.33 (bs, 5H), 8.03 (s, 1H), 12.84 (bs, 1H). 2) 6-(3-Acetoxypropyl)- thieno[2,3-d]pyrimidin-4(3H)-one (4-A26): A mixture of ethyl 2-amino-5-(3-acetyloxypropyl)-thiophene-3-carboxylate (2.6 g, 9.7 mmole), ammonium acetate (0.74 g, 9.7 mmole) and formamide (8.64 ml, 19.2 mmole), was stirred under reflux at 145°C for 12 hours. It was then cooled, diluted with water (20 ml), extracted with ethyl acetate (3 x 25 ml), dried, concentrated and purified by column chromatography to obtain the pure 6-(3-Acetoxypropyl)- thieno[2,3-d]pyrimidin-4(3H)-one of Formula (4-A26) (1.8 gm, 75%). 1HNMR (CDC13, 200 MHz): 1.94-2.18 (m including s at 2.07, 5H), 2.85-3.08 (m, 2H), 4.05-4.30 (m, 2H), 7.18 (s,lH), 8.03 (s, 1H), 12.63 (bs, 1H). 3)5,6,7,8-Tetrahydrobenzothieno[2,3-d]pyrimidin-4(3H)-one(4-A09): A mixture of ethyl 2-amino-4, 5, 6, 7-tetrahydrobenzo[b]thiophene-3-carboxylate (0.7 g, 3.1 mmole), ammonium acetate (0.31 g, 4.04 mmole) and formamide (0.67 ml, 16.8 mmole), was stirred under reflux at 140°C for 13 hours. It was then cooled, diluted with water (20 ml), extracted with ethyl acetate (3 x 35 ml), dried, concentrated and purified by column chromatography to obtain the pure 5,6,7,8-tetrahydrobenzothieno[2,3-d]pyrimidin-4(3H)-one of Formula (4-A09) (0.53 gm, 82%). 1HNMR (CDC13 + DMSO-d6, 200 MHz): 1.36-1.52 (m, 4H), 2.31-2.40 (m, 2H), 2.51-2.62 (m, 2H), 7.45 (s, 1H). 4) 6-(4-Benzyloxybutyl)-thieno[2,3-d]pyrimidin-4(3H)-one (4-A01): lHNMR (CDC13, 200 MHz): 1.61-1.92 (m, 4H), 2.89 (t, J=6 Hz, 2H), 3.51 (t, J=6 Hz, 2H), 4.51 (s, 2H), 7.17 (s, 1H), 7.34 (bs, 5H), 8.02 (s, 1H), 12.54 (bs, 1H). 5) 6-(n-Hexyl)-thieno[2,3-d]pyrimidin-4(3H)-one (4-A03): 1HNMR (CDC13, 200 MHz): 0.90 (t, J=6 Hz, 3H), 1.21-1.50 (m, 6H), 1.61-1.86 (m, 2H), 2.87 (t, J=8 Hz, 2H), 7.15 (s, 1H), 8.03 (s, 1H), 12.80 (bs, 1H). 6) 6-(n-Pentyl)-thieno[2,3-d]pyrimidin-4(3H)-one (4-A04): lHNMR (CDC13, 200 MHz): 0.89 (t, J=6 Hz, 3H), 1.16-1.45 (m, 4H), 1.52-1.83 (m, 2H), 2.84 (t, J=8 Hz, 2H), 7.13 (s, 1H), 8.07 (s, 1H), 12.90 (bs, 1H). 7) 5-n-Butyl- -6-(n-propyl)- thieno[2,3-d]pyrimidin-4(3H)-one (4-A05): lHNMR (CDC13, 200 MHz): 0.93 (t, J=6 Hz, 3H), 0.99 (t, J=6 Hz, 3H), 1.26-1.85 (m, 6H), 2.79 (t, J=6 Hz, 2H), 2.95 (t, J=6 Hz, 2H), 7.95 (s, 1H), 12.34 (bs, 1H). 8) 6-(n-Heptyl)- thieno[2,3-d]pyrimidin-4(3H)-one (4-A06): lHNMR (CDC13, 200 MHz): 0.89 (t, J=6 Hz, 3H), 1.26-1.38 (m, 8H), 1.60-1.78 (m, 2H), 2.87 (t, J=6 Hz, 2H), 7.17 (s, 1H), 8.05 (s, 1H), 12.82 (bs, 1H). 9) 3,5,6,7-Tetrahydrocyclopenta[4,5]thieno[2,3-d]pyrimidin-4(3H)-one (4-A07): The crude compound obtained was used as such for further reaction. 10) 6-Methyl-5-n-pentyl-thieno[2,3-d]pyrimidin-4(3H)-one (4-A08): lHNMR (CDC13, 200 MHz): 0.91 (bt, J=6 Hz, 3H), 1.25-1.50 (m, 4H), 1.52-1.68 (m, 2H), 2.43 (s, 3H), 2.93 (t, J=8 Hz, 2H), 7.96 (s, 1H), 12.32 (bs, 1H). 11) 6-n Hexyl-5-methyl - -thieno[2,3-d]pyrimidin-4(3H)-one (4-A10): lHNMR (CDC13, 200 MHz): 0.90 (t, J=6 Hz, 3H), 1.22-1.46 (m, 6H), 1.52-1.76 (m, 2H), 2.52 (s, 3H), 2.78 (t, J=6 Hz, 2H), 7.96 (s, 1H), 12.32 (bs, 1H). 11) 5-Methyl-6-n-pentyl-thieno[2,3-d]pyrimidin-4(3H)-one (4-A11): lHNMR (CDC13, 200 MHz): 0.91 (t, J=6 Hz, 3H), 1.25-1.48 (m, 4H), 1.55-1.75 (m, 2H), 2.52 (s, 3H), 2.79 (t, J=8 Hz, 2H), 8.20 (s, 1H). 12) 6-(7-Acetoxyheptyl)- thieno[2,3-d]pyrimidin-4(3H)-one (4-A12): lHNMR (CDC13, 200 MHz): 1.24-1.42 (m, 6H), 1.48-1.77 (m, 4H), 1.97 (s, 3H), 2.79 (t, J=8 Hz, 2H), 3.98 (t, J=7 Hz, 2H), 7.08 (s, 1H), 8.03 (s, 1H). 13) 5-(2-Phenylethyl)-thieno[2,3-d]pyrimidin-4(3H)-one (4-A14): lHNMR (CDC13 + DMSO-d6, 200 MHz): 3.05 (t, J=7 Hz, 2H), 3.34 (t, J=7 Hz, 2H), 6.84 (s, 1H), 7.30 (bs, 5H), 8.00 (s, 1H). 14) 6-Benzyl-5-methyl-thieno[2,3-d]pyrimidin-4(3H)-one (4-A15): lHNMR (DMSOd6,200 MHz): : 2.48 (s, 3H), 4.13 (s, 2H), 7.22-7.34 (m, 5H), 8.00 (s, 1H). 15) 6-(n-Decyl)-thieno[2,3-d]pyrimidin-4(3H)-one (4-A16): lHNMR (CDC13, 200 MHz): 0.88 (t, J=6 Hz, 3H), 1.18-1.42 (m, 14H), 1.62-1.83 (m, 2H), 2.86 (t, J=6 Hz, 2H), 7.17 (s, 1H), 8.15 (s, 1H). 16) 6-(n-Nonyl)-thieno[2,3-d]pyrimidin-4(3H)-one (4-A 17): lHNMR (CDC13, 200 MHz): 0.91 (t, J=6 Hz, 3H), 1.14-1.55 (m, 12H), 1.65-1.92 (m, 2H), 2.89 (t, J=6 Hz, 2H), 7.19 (s, 1H), 8.09 (s, 1H), 12.96 (bs, 1H). 17) 6-(n-Propyl)-thieno[2,3-d]pyrimidin-4(3H)-one (4-A18): lHNMR (CDC13, 200 MHz): 1.01 (t, J=6 Hz, 3H), 1.67-1.85 (m, 2H), 2.84 (t, J=6 Hz, 2H), 7.16 (s, 1H), 8.05 (s, 1H), 12.74 (bs, 1H). 18) 7,8,9,10,11,12,13,14,15,16-Decahydrocyclododeca[4,5]thieno[2,3-d]pyrimidin-4(3H)-one(4-A19): lHNMR (CDC13, 200 MHz): 1.21-1.58 (m, 12H), 1.68-2.01 (m, 4H), 2.79-2.99 (m, 4H), 7.98 (s, 1H), 12.08 (bs, 1H). 19) 5-Methyl-6-n-octyl-thieno[2,3-d]pyrimidin-4(3H)-one (4-A20): 1HNMR (CDC13, 200 MHz): 0.92 (t, J=7 Hz, 3H), 1.20-1.52 (m, 10H), 1.60-1.75 (m, 2H), 2.55 (s, 3H), 2.82 (t, J=8 Hz, 2H), 8.19 (s, 1H). 20) 6-n-Butyl-5-methyl-thieno[2,3-d]pyrimidin-4(3H)-one (4-A21): lHNMR (CDC13, 200 MHz): 0.96 (t, J=6 Hz, 3H), 1.32-1.73 (m, 4H), 2.52 (s, 3H), 2.79 (t, J=8 Hz, 2H), 7.99 (s,lH), 12.48 (bs, 1H). 21) 6-Ethyl-thieno[2,3-d]pyrimidin-4(3H)-one (4-A22): 1HNMR (CDC13, 200 MHz): 1.39 (t, J=8 Hz, 3H), 2.92 (q, J=8 Hz, 2H), 7.17 (s, 1H), 8.02 (s, 1H). Example 6 General methods of preparation of compounds of Formula (3): Method A: A mixture of ethyl cyanoacetate (1 eq), sulphur (1 eq), triethyl amine (0.5 eq) and a ketone or aldehyde (1 eq) was stirred at 30 to 80°C for 8 to 20 hrs, cooled, diluted with water, extracted with ethyl acetate, dried, concentrated and purified by column chromatography to obtain the pure compounds of the Formula (3). Method B: A mixture of ethyl cyanoacetate (1 eq), sulphur (1 eq), morpholine (1 eq) and ketone or aldehyde (1 eq) in ethanol was stirred at 30 to 60°C for 5 to 20 hrs, ethanol was removed on rotavapor, the reaction mixture was extracted with ethyl acetate, dried, concentrated and purified by column chromatography to get the pure compounds of the Formula (3). 1. Ethyl 2-amino-5-(3-benzyloxypropyl)-thiophene-3-carboxylate (3-A02): A mixture of ethyl cyanoacetate (2.77 ml, 26 mmol), sulphur (0.83 g, 26 mmol), triethyl amine (1.82 ml, 13 mmol) and 5-benzyloxy-l-pentanal (5.00 g, 26 mmol) in DMF (40 ml) was stirred at45-50°C for 12 hours. It was then cooled, diluted with water (100 ml), extracted with ethyl acetate (2 x 100 ml), dried, concentrated and purified by column chromatography to obtain the pure ethyl 2-amino-5-(3-benzyloxypropyl)-thiophene-3-carboxylate (4.5 gm, 54%). HNMR (CDC13, 200 MHz): 1.34 (t, J=8 Hz, 3H), 1.80-1.96 (m, 2H), 2.70 (t, J=7 Hz, 2H), 3.51 (t, J=7 Hz, 2H), 4.25 (q, J=7 Hz, 2H), 4.51 (s, 2H), 5.80 (bs, 2H), 6.64 (s, 1H), 7.34 (bs, 5H). 2. Ethyl 2-amino-4, 5, 6, 7-tetrahydrobenzo[b]thiophene-3-carboxylate (3-A09): A mixture of ethyl cyanoacetate (1.15 g, 0.0lmol), sulphur (0.32 g, 0.01 mol), triethyl amine (0.52 g, 0.005 mol) and cyclohexanone (1.0 g, 0.01 mol) in DMF (10 ml) was stirred at 55 °C for 12 hours. It was cooled, diluted with water (80 ml), extracted with ethyl acetate (2 x 100 ml), dried, concentrated and purified by column chromatography to obtain the pure ethyl 2-amino-4, 5, 6, 7-tetrahydrobenzo[b]thiophene-3-carboxylate of Formula (3-A09) (1.13 gm, 50%). lHNMR (CDC13, 200 MHz): 1.27 (t, J=7 Hz, 3H), 1.62-1.78 (m, 4H), 2.35-2.50 (m, 2H), 2.54-2.70 (m, 2H), 4.19 (q, J=7 Hz, 2H). 3. Ethyl 5-(3-acetoxypropyl)-2-aminothiophene-3-carboxylate (3-A26): A mixture of ethyl cyanoacetate (6.2 ml, 50 mmol), sulphur (4.6 g, 50 mmol), morpholine (4.3 ml, 50 mmol) and 5-acetoxy-l-pentanal (8 g, 50 mmol) in ethanol (25 ml) was stirred at 80°C for 12 hours. Ethanol was removed on rotavapor, the reaction mixture was diluted with water (100 ml), extracted with ethyl acetate (3 x 100 ml), dried, concentrated and purified by column chromatography to get the pure ethyl 5-(3-acetoxypropyl)-2-amino- thiophene-3- carboxylate (6.4 gm, 42.5%). lHNMR (CDC13, 200 MHz): 1.32 (t, J=7 Hz, 2H), 1.81-1.98 (m, 2H), 2.05 (s, 3H), 2.65 (t, J=7 Hz, 2H), 4.08 (t, J=7 Hz, 2H), 4.24 (q, J=7 Hz, 2H), 5.18 (bs, 2H), 6.64 (s, IH). The methods described above were used for preparing more compounds some of which are given below: 4. Ethyl 2-amino-5-(4-benzyloxybutyl)-thiophene-3-carboxylate (3-A01): 1HNMR (CDC13, 200 MHz): 1.33 (t, J=8 Hz, 3H), 1.60-1.75 (m, 4H), 2.59 (bt, J=6 Hz, 2H), 3.48 (bt, J=6 Hz, 2H), 4.25 (q, J=8 Hz, 2H), 4.50 (s, 2H), 5.77 (bs, 2H), 6.62 (s, IH), 7.33 (bs, 5H). 5. Ethyl 2-amino-5-n-hexyl-thiophene-3-carboxylate (3-A03): 1HNMR (CDC13, 200 MHz): 0.90 (bt, J=6 Hz, 3H), 1.22-1.42 (m, 9H), 1.49-1.63 (m, 2H), 2.57 (t, J=7 Hz, 2H), 4.26 (q, J=7 Hz, 2H), 5.79 (bs, 2H), 6.61 (s, IH). 6. Ethyl 2-amino-5-n-pentyl-thiophene-3-carboxylate (3-A04): lHNMR (CDC13, 200 MHz): 0.88 (bt, J=6 Hz, 3H), 1.21-1.40 (m, 7H), 1.49-1.71 (m, 2H), 2.55 (t, J=8 Hz, 2H), 4.24 (q, J=7 Hz, 2H), 5.65 (bs, 2H), 6.61 (s, IH). 7. Ethyl 2-amino-5-n-heptyl-thiophene-3-carboxylate (3-A06): lHNMR (CDC13, 200 MHz): 0.89 (bt, J=6 Hz, 3H), 1.26-1.48 (m, 11H), 1.51-1.71 (m, 2H), 2.58 (t, J=8 Hz, 2H), 4.26 (q, J=7 Hz, 2H), 5.49 (bs, 2H), 6.63 (s, IH). 8. Ethyl 2-amino-5, 6-dihydro-4H-cyclopenta[b]thiophene-3-carboxylate (3-A07): 1HNMR (CDC13, 200 MHz): 1.32 (t, J=7 Hz, 3H), 2.22-2.38 (m, 2H), 2.65-2.90 (m, 4H), 4.24 (q, J=7 Hz, 2H), 5.85 (bs, 2H). 9. Ethyl 2-amino-5-methyl-4-(n-pentyl)-thiophene-3-carboxylate (3-A08): 1HNMR (CDC13, 200 MHz): 0.91 (t, J=6 Hz, 3H), 1.30-1.52 (m, 7H), 2.16 (s, 3H), 2.35-2.50 (m, 2H), 2.55-2.70 (m, 2H), 4.29 (q, J=7 Hz, 2H), 5.92 (bs, 2H). 10. Ethyl 2-amino-5-n-hexyl-4-methyl-thiophene-3-carboxylate (3-A10): lHNMR (CDC13, 200 MHz): 0.90 (bt, J=6 Hz, 3H), 1.22-1.40 (m, 9H), 1.45-1.63 (m, 2H), 2.18 (s, 3H), 2.54 (t, J=8 Hz, 2H), 4.28 (q, J=8 Hz, 2H), 5.01 (bs, 2H). 11. Ethyl 2-amino-5(7-acetoxy-n-heptyl)-thiophene-3-carboxylate (3-A12): lHNMR (CDC13, 200 MHz): 1.21-1.40 (m, 9H), 1.45-1.67 (m, 4H), 2.00 (s, 3H), 2.52 (t, J=8 Hz, 2H), 4.00 (t, J=6 Hz, 2H), 4.20 (q, J=8 Hz, 2H), 5.67 (bs, 2H), 6.57 (s, 1H). 12. Ethyl 2-amino-5-(2-phenylethyl)-thiophene-3-carboxylate (3-A14): lHNMR (CDC13, 200 MHz): 1.35 (t, J=8 Hz, 3H), 2.74-3.07 (m, 4H), 4.32 (q, J=8 Hz, 2H), 5.19 (bs, 2H), 7.15-7.26 (m, 6H). 13. Ethyl 2-amino-5-benzyl-4-methyl-thiophene-3-carboxylate (3-A15): lHNMR (CDC13, 200 MHz): 1.35 (t, J=8 Hz, 3H), 2.25 (s, 3H), 3.90 (s, 2H), 4.29 (q, J=7 Hz, 2H), 5.18 (bs,2H), 7.19 (bs, 5H). 14. Ethyl 2-amino-5-n-decyl-thiophene-3-carboxylate (3-A16): lHNMR (CDC13, 200 MHz): 0.88 (bt, J=6 Hz, 3H), 1.18-1.40 (m including t at 1.33 with J=7 Hz, 17H), 1.49-1.65 (m, 2H), 2.56 (t, J=7 Hz, 2H), 4.25 (q, J=7 Hz, 2H), 5.40 (bs, 2H), 6.63 (s, 1H). 15. Ethyl 2-amino-5-n-nonyl-thiophene-3-carboxylate (3-A17): lHNMR (CDC13, 200 MHz): 0.88 (bt, J=7 Hz, 3H), 1.15-1.42 (m including tat 1.32 with J=7 Hz, 15H), 1.47-1.65 (m, 2H), 2.54 (t, J=7 Hz, 2H), 4.24 (q, J=7 Hz, 2H), 5.78 (bs, 2H), 6.61 (s, 1H). 16. Ethyl 2-amino-5-n-propyl-thiophene-3-carboxylate (3-A18): lHNMR (CDC13, 200MHz): 0.95 (t, J=7 Hz, 3H), 1.34 (t, J=7 Hz, 3H), 1.51-1.71 (m, 2H), 2.56 (t, J=7 Hz, 2H), 4.26 (q, J=7 Hz, 2H), 4.75 (bs, 2H), 6.64 (s, 1H). 17. Ethyl 2-amino-4,5,6,7,8,9,10,l l,12,13-decahydro-[l]cyclododeca[b]thiophene-3-carboxylate(3-A19): lHNMR(CDC13, 200 MHz): 1.21-1.50 (m, 15H), 1.55-1.71 (m, 4H), 2.54-2.71 (m, 4H), 4.27 (q, J=7 Hz, 2H). 18. Ethyl 2-amino-5-ethyl-thiophene-3-carboxylate (3-A22): lHNMR (CDC13, 200 MHz): 1.23 (t, J=7 Hz, 3H), 1.34 (t, J=7 Hz, 3H), 2.62 (q, J=7 Hz, 2H), 4.26 (q, J=7 Hz, 2H), 4.62 (bs, 2H), 6.64 (s, 1H). Example 7 Antifungal Activity Testing: The compounds of Formula 1 are antifungal agents effective against Candida albicans. In vitro evaluation of antifungal activity was performed by determining the minimum inhibitory concentration (MIC). Anti-fungal susceptibility testing of these anti-fungal compounds was done by broth dilution method using RPMI 1640 medium with MOPS buffer. Known anti-fungal agents like fluconazole and amphotericin-B were used as positive control. End points were determined after 48 hours visually and by using spectrophotometer wherever necessary. Different dilutions were tried and various sets of experiments performed. The activity parameters are enumerated in Table 1: Table 1: MIC obtained by broth macro-dilution method No. Code no. StructureRl=R2=2,4-difluoro MIC against fungi in ug/ml C. albicans (ATCC 24433) A. aigcr (ATCC 16404) F. prolifcmtum (ATCC 10052) Fluconaz ole 0.25-1 M-12S >123 Ampliote ricin B 0.12-0.25 0.25-1 1-2 01 1-A01 R3=-(CHi>40Bn, R4=H 0.06-0.12 XI till 4 XI till 4 02 1-A02 R3=-(CH;bOBu, R4=H 0.06-0.12 XI till 4 XI till 4 03 1-A03 R3=-(CH;);Me, R4=H 0.03-0.06 XI till 2 XI till 2 04 1-A04 R3-(CFfc)*Me, R4=H 0.03-0.06 XI till 4 XI till 4 05 1-A05 R3=-(CH2)-Me, R4= -(CHi)sMe 2-4 XI till 4 XI till 4 06 1-A06 R3«-(CH;)6.Me, R4=H 0.06-0.12 XI till 2 XI till 2 07 1-A07 R3, R4= -fCH;),. 025-0.5 XI tvU 2 XI till 2 08 1-AOS R3=-Me, R4= I.CH;)*Me 2-4 XI till 4 XI till 4 09 1-A09 R3, R4= -fCHi)* 025-0.5 XI hfl S XI till S 10 1-A10 R3=-(CH2)5Me, R4= -Me i-"> XI till 2 XI till 2 11 1-A11 R3—(CHzkMe, R4= -Me 1-2 NI till 2 XI till 2 12 1-A12 R3=-(CHi)rOAc, R4= H 0.12-0.25 XI till 2 XI till 2 13 1-A13 R3=-(CH-)-OH, R4= H 0.12-0.25 XI till 16 XI till 16 14 1-A14 R3= H, R4=(CH:):Fh 0.5-1 XI till 2 XI till 2 15 1-A15 R3- CHsPh, R4= CHs 1-2 XI till 4 XI till 4 16 1-Alb R3= (CHz)oCHj. R4= H 1-2 XI hll 2 XI till 2 17 1-A17 R3= (CH:)sCHj. R4= H 0.25-0,5 XI till 4 XI till 4 IS 1-A1S R3= (CHihCHj. R4= H 0.06-0.12 XI hll 32 XI till 32 19 1-A19 R3, R4= (CH:)io XI till 2 XI till 2 XI till 2 20 1-A22 R3- CHJCHJ. R4= H 0.06-0.12 XI till 16 XI till 16 21 1-A23 R3= -fCH^OH R4= H 1-2 XI till 64 XI till 64 22 1-A24 R3=(CH;}*OCOCHi-NHBoc. R4= H 0.5-1 XI till 16 XI till 16 23 1-A25 R3=(CHi)*OCOCH=NH: , R4=H 4-S XI hll 8 XI Hll 8 24 1-A26 R3= -(CHi'JsOAc, R4= H 1-2 XI till 64 XI till 64 25 1-A27 R3= -(CHi}3OH R4= H 2-4 XI till 128 XI till 128 2b 1-A2S R3-CH»R4-H 025-0.5 XI till 64 XI till 64 It will be evident to those skilled in the art that the invention is not limited to the details of the foregoing illustrative examples and that the present invention may be embodied in other specific forms without departing from the essential attributes thereof, and it is therefore desired that the present embodiments and examples be considered in all respects as illustrative and not restrictive, reference being made to the appended claims, rather 47 than to the foregoing description, and all changes which come within the meaning and range of equivalency of the claims are therefore intended to be embraced therein. 48 We claim 1. Antifungal compounds of the Formula (1): R2 1 wherein, Rl is hydrogen or a halogen selected from fluorine, chlorine, bromine or iodine; R2 is hydrogen or a halogen selected from fluorine, chlorine, bromine or iodine; R3 and R4 which may be the same or different and each represents a hydrogen, alkyl group of linear or branched chain of 1 to 20 carbon atoms optionally substituted with aryl group, hydroxy 1 group, alkanoate group, acetoxy group, amino acetyloxy group, N-Boc- amino acetyloxy group, alkoxy (-OR) group (wherein R= alkyl group with 1 to 4 carbon atoms), benzyloxy, arylalkyl group (wherein the aryl group is phenyl which is either unsubstituted or substituted with alkyl group of 1 to 3 carbon atoms) or cycloalkyl group with 3 to 10 carbon atoms; the streochemically isomeric forms or a pharmaceutical ly acceptable salt thereof. 2. A process of preparing compounds of Formula'(l) comprising: a) preparing 2-amino-4 and/or 5-substituted thiophene-3-carboxylates of Formula (3) wherein R is methyl or ethyl and R3 and R4 are as defined above by Gewald synthesis; b) contacting 2-amino-4 and/or 5- substituted thiophene-3-carboxylate of Formula (3) with formamide and ammonium acetate to obtain the thieno-[2, 3-d]-pyrimidin-4(3H)-one of Formula (4) wherein Rl and R2 are as defined above; and c) treating the compound of Formula (4) with epoxide of Formula (5), where Rl and R2 are as defined above in presence of a base to obtain the compound of the Formula (1). 3. A compound according to claim 1 selected from the group consisting of: 6-(4-Benzyloxybutyl)-3-[2-(2,4-difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l- ylpropyl]-thieno[2,3-d]pyrimidin-4(3H)-one: 6-(4-Benzyloxypropyl)-3-[2-(2,4-difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l- ylpropyl]-thieno[2,3-d]pyrimidin-4(3H)-one: 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-(n-hexyl)- thieno[2,3-d]pyrimidin-4(3H)-one: 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-n- pentylthieno[2,3-d]pyrimidin-4(3H)-one: 5-n-Butyl-3-[2-(2,4-difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-n- propyl-thieno[2,3-d]pyrimidin-4(3H)-one: 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-n- heptylthieno[2,3-d]pyrimidin-4(3H)-one: 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-3,5,6,7- tetrahydrocyclopenta[4,5]thieno[2,3-d]pyrimidin-4(3H)-one: 3-[2-(2,4-Difluorophenyl)- 2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]- 6-methyl-5- npentyl-thieno[2,3-d]pyrimidin-4(3H)-one: 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[ 1,2,4]triazol-1 -yl-propyl]-5,6,7,8- tetrahydrobenzothieno[2,3-d]pyrimidin-4(3H)-one: 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-n-hexyl-5- methyl-thieno[2,3-d]pyrimidin-4(3H)-one: 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-n-hexyl-5- methyl-thieno[2,3-d]pyrimidin-4(3H)-one: 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-5-methyl-6- npentyl-thieno[2,3-d]pyrimidin-4(3H)-one 6-(7-Acetoxyheptyl)-3-[2-(2,4-difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl- propyl]-thieno[2,3-d]pyrimidin-4(3H)-one: 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-(7-hydroxy heptyl)-thieno[2,3-d]pyrimidin-4(3H)-one: 3-[2-(2, 4-Difluorophenyl)-2-hydroxy-3-[l, 2, 4] triazol-l-yl-propyl]-5(2- phenylethyl)-thieno[2,3-d]pyrimidin-4(3H)-one: 6-Benzyl-3-[2-(2,4-difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-5- methyl-thieno[2,3-d]pyrimidin-4(3H)-one: 6-n-Decyl-3-[2-(2, 4-difluorophenyl)-2-hydroxy-3-[l, 2, 4] triazol-1-yl-propyl]- thieno [2,3-d] pyrimidin-4(3H)-one: 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-n- nonylthieno [2,3-d] pyrimidin-4(3H)-one: 3-[2-(2, 4-Difluorophenyl)-2-hydroxy-3-[1, 2, 4] triazol-l-yl-propyl]-6-(n- propyl)-thieno[2,3-d]pyrimidin-4(3H)-one: 3-[2-(2, 4-Difluorophenyl)-2-hydroxy-3-[l, 2, 4] triazol-1-yl-propyl]- 3,5,6,7,8,9,10,11,12,13,14-undecahydrocyclododeca[4,5]thieno[2,3-d]pyrimidin- 4(3H)-one: 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]- 5-methyl- 6-n- octyl-thieno[2,3-d]pyrimidin-4(3H)-one: 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-n-butyl-5- methyl-thieno[2,3-d]pyrimidin-4(3H)-one: 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-ethylthieno[ 2,3-d]pyrimidin-4(3H)-one: 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-(4- hydroxybutyl)-thieno[2,3-d]pyrimidin-4(3H)-one: 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-(4-N- Bocaminoacetyloxybutyl)-thieno[2,3-d]pyrimidin-4(3H)-one: 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-(4- aminoacetyloxybutyl)-thieno[2,3-d]pyrimidin-4(3H)-one: 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-(3- acetoxypropyl)-thieno[2,3-d]pyrimidin-4(3H)-one: 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6-(3- hydroxypropyl)-thieno[2,3-d]pyrimidin-4(3H)-one: 3-[2-(2,4-Difluorophenyl)-2-hydroxy-3-[l,2,4]triazol-l-yl-propyl]-6- methylthieno[2,3-d]pyrimidin-4(3H)-one. 4. A pharmaceutical composition comprising antifungal compound of formula (1) according to any one of the claims 1 to 3, in association with at least one pharmaceutical excipient. 5. A method for treating or preventing a fungal infection in a subject, which method comprises administering an effective amount of the compound of formula (1) in association with pharmaceutical excipients. 6. Use of a compound of formula (1) according to any one of the claims 1 to 3, for the preparation of medicament useful for the treatment or prevention of fungal infections. ABSTRACT The present invention discloses novel compounds of the Formula (1), containing thieno-[2,3-d]pyrimidin-4(3H)-one moieties and pharmaceutically acceptable salts thereof, methods for preparing these compounds, the use of these compounds in prevention and treatment of fungal infections, and pharmaceutical preparations containing these novel compounds.

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