Title of Invention	A PROCESS FOR PREPARATION OF NEBIVOLOL AND INTERMEDIATE FOR IT
Abstract	The invention discloses process for the preparation of 2H-1-benzopyran-2-methanol, a, a' [iminobis(methylene)]bis[6-fluoro-3,4-dihydro-,[2R[R(S*)]]]] i.e. nebivolol lof formula (IX) or its pharmaceutically acceptable salts comprising the steps of: (a) reacting 6-fluoro-3,4-dihydro-2H-1-benzopyran-2-carboxylic acid with an acid activating agent, and an amine RR'NH, wherein R and R' are independently lH, alkyl or aryl, optionally joined together with or without a heteroatom selected from O, N and S, to give 6-fluoro-3,4-dihydro-2H-1-benzopyran-2-carboxylic amide; (b) reducing the said amide by using alkoxy metallic hydride to give 6-fluro-3, 4-dihydro-2H-1-benzopryan-2-carboxaldehyde; (c) converting the said intermediate into nebivolol of formula (IX) in a known manner, and (d) optionally converting nebivolol thus obtained into the pharmaceutically acceptable salt thereof.

Title of Invention

A PROCESS FOR PREPARATION OF NEBIVOLOL AND INTERMEDIATE FOR IT

Abstract

The invention discloses process for the preparation of 2H-1-benzopyran-2-methanol, a, a' [iminobis(methylene)]bis[6-fluoro-3,4-dihydro-,[2R*[R*(S*)]]]] i.e. nebivolol lof formula (IX) or its pharmaceutically acceptable salts comprising the steps of: (a) reacting 6-fluoro-3,4-dihydro-2H-1-benzopyran-2-carboxylic acid with an acid activating agent, and an amine RR'NH, wherein R and R' are independently lH, alkyl or aryl, optionally joined together with or without a heteroatom selected from O, N and S, to give 6-fluoro-3,4-dihydro-2H-1-benzopyran-2-carboxylic amide; (b) reducing the said amide by using alkoxy metallic hydride to give 6-fluro-3, 4-dihydro-2H-1-benzopryan-2-carboxaldehyde; (c) converting the said intermediate into nebivolol of formula (IX) in a known manner, and (d) optionally converting nebivolol thus obtained into the pharmaceutically acceptable salt thereof.

Full Text

Documents:

246-KOL-2003-CORRESPONDENCE.pdf

246-KOL-2003-FORM-27.pdf

246-kol-2003-granted-abstract.pdf

246-kol-2003-granted-assignment.pdf

246-kol-2003-granted-claims.pdf

246-kol-2003-granted-correspondence.pdf

246-kol-2003-granted-description (complete).pdf

246-kol-2003-granted-examination report.pdf

246-kol-2003-granted-form 1.pdf

246-kol-2003-granted-form 18.pdf

246-kol-2003-granted-form 2.pdf

246-kol-2003-granted-form 3.pdf

246-kol-2003-granted-form 5.pdf

246-kol-2003-granted-gpa.pdf

246-kol-2003-granted-letter patent.pdf

246-kol-2003-granted-reply to examination report.pdf

246-kol-2003-granted-specification.pdf

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Patent Number

221733

Indian Patent Application Number

246/KOL/2003

PG Journal Number

27/2008

Publication Date

04-Jul-2008

Grant Date

03-Jul-2008

Date of Filing

28-Apr-2003

Name of Patentee

TORRENT PHARMACEUTICALS LTD.

Applicant Address

CENTRAL PLAZA, 1ST FLOOR, ROOM # - 106, 2/6 SARAT BOSE ROAD, CALCUTTA-700020

Inventors:

#	Inventor's Name	Inventor's Address
1	NADKARNI SUNIL SADANAND	TORRENT PHARMACEUTICALS LIMITED, TORRENT RESEARCH CENTRE, P.O. BHAT 382 428, DIST. GANDHINAGAR
2	SRINIVASARAO ATTANTI VEERA VENKATA	TORRENT PHARMACEUTICALS LIMITED, TORRENT RESEARCH CENTRE, P.O. BHAT 382 428, DIST. GANDHINAGAR
3	PATEL HASMUKH MATHURBHAI	TORRENT PHARMACEUTICALS LIMITED, TORRENT RESEARCH CENTRE, P.O. BHAT 382 428, DIST. GANDHINAGAR

PCT International Classification Number

C07D 407/12

PCT International Application Number

N/A

PCT International Filing date

PCT Conventions:

#	PCT Application Number	Date of Convention	Priority Country
1			NA