| Title of Invention | AN IMPROVED PROCESS FOR MANUFACTURE OF (2S,3aS,7aS)-1-[(2S)-2-[[(1S)-1-(ETHOXYCARBONYL)BUTYL]AMINO]-1-OXOPROPYL]OCTAHYDRO-1H-INDOLE-2-CARBOXYLIC ACID AND ITS TERT. BUTYL AMINE SALT |
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| Abstract | The present invention discloses a process for the synthesis and isolation of (2S, 3aS, 7aS)-1-[(2S)-2-[[(1S)-1-(ethoxycarbonyl)butyl]amino]-1-oxopropyl]octahydro-1H-indole-2-carboxylic acid and its tert. butylamine salt, by condensing (2S,3aS, 7aS)-octahydroindole-2-carboxylic acid benzyl ester and N-[(S)-1-carboxybutyl]-(S)-alanine ethyl ester in non-reactive solvents in turn avoiding the formation of impurity viz. N-acetyl (2S,3aS,7aS)-octahydroindole-2-carboxylic acid benzyl ester (Formula V). The de-protection of benzyl ester group is optimized and then isolation of the product from aqueous layer by extraction using an organic solvent, which eliminates the need of lyophilization. The process of the present invention yields perindopril erbumine salt of Formula 1B free of contaminants derivable from diclohexylcarbodiimide and impurities originated by the use of ethyl acetate. |
| Full Text | N/A |
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566-mum-2004-abstract(31-05-2005).doc
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| Patent Number | 231512 | |||||||||||||||||||||||||||||||||
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| Indian Patent Application Number | 566/MUM/2004 | |||||||||||||||||||||||||||||||||
| PG Journal Number | 13/2009 | |||||||||||||||||||||||||||||||||
| Publication Date | 27-Mar-2009 | |||||||||||||||||||||||||||||||||
| Grant Date | 05-Mar-2009 | |||||||||||||||||||||||||||||||||
| Date of Filing | 31-May-2004 | |||||||||||||||||||||||||||||||||
| Name of Patentee | M/S. IPCA LABORATORIES LIMITED | |||||||||||||||||||||||||||||||||
| Applicant Address | 48, KANDIVLI INDUSTRIAL ESTATE, MUMBAI-400067 | |||||||||||||||||||||||||||||||||
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| PCT International Classification Number | C07D503/00 | |||||||||||||||||||||||||||||||||
| PCT International Application Number | N/A | |||||||||||||||||||||||||||||||||
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