New process for the synthesis of perindopril and its pharmaceutically acceptable salts

摘要

Disclosed is the process for the synthesis of the compound of formula (I) and its pharmaceutically acceptable salts thereof characterised in that a compound of formula (II) wherein R1 represents a hydrogen atom or a benzyl or linear or branched (C1-6)alkyl group, is reacted with a compound of formula (III) having an S configuration wherein X represents a halogen atom and R2 represents a protecting group for the amino function, in the presence of a base, to yield, after deprotection of the amino function, a compound of formula (IV) wherein R1 is as defined hereinbefore, which is reacted with a compound of formula (V) wherein G represents a chlorine, bromine or iodine atom or a p-toluenesulfonyloxy, methanesulfonyloxy of trifluoromehtansulfonyloxy group, in the presence of a base, to yield a compound of formula (VI) wherein R1 is as defined hereinbefore, which is hydrogenated in the presence of a catalyst such as palladium, platinum, rhodium or nickel to yield, after deprotection where necessary, the compound of formula (I).