PROCESS FOR SYNTHESIS OF (2S, 3AS, 7AS) - PERHYDROINDOL-2-CARBOXYLIC ACID AND ITS ESTERS, USE IN THE SYNTHESIS OF PERINDOPRIL

摘要

Production of (2S,3aS,7aS)-perhydroindole-2-carboxylic acid derivatives (I) comprises reacting 1-(1-cyclohexenyl)pyrrolidine (III) with a N-protected 3-iodoalanine derivative (IV), deprotecting the amino group, cyclizing and dehydrating the product, catalytically hydrogenating the product at 1-30 bar, and optionally deprotecting or reprotecting the acid group. Production of compounds of formula (I) comprises reacting 1-(1-cyclohexenyl)pyrrolidine (III) with a N-protected 3-iodoalanine compound of formula (IV) to give a product of formula (V), deprotecting the amino group and cyclizing and dehydrating the product to give a compound of formula (VI), and catalytically hydrogenating (VI) at 1-30 bar and optionally deprotecting or reprotecting the acid group. R = H or a protecting group, and R' = a protecting group. An Independent claim is also included for production (unspecified) of perindopril or its salts from (I) produced as above.