NEW ACID SYNTHESIS PROCEDURE (2S, 3AS, 7AS) -PERHYDROINDOL-2-CARBOXYL AND ITS ETERES AND ITS APPLICATION TO PERINDROPIL SYNTHESIS.

摘要

Method of synthesis of the compounds of Formula (I), in which R represents a hydrogen atom or a group protecting the acid function, characterized in that 1- (1-cyclohexen-1-yl) pyrrolidine of Formula ( III), with the compound of Formula (IV): in which R is as defined in Formula (I) and R ¿represents a protective group of the amine function other than R, to lead to the compound of Formula ( V), in which R and R ¿are as defined above, from which the amine function is deprotected before cyclization followed by dehydration, to lead to the compound of Formula (VI), in which R is such as defined above, which is subjected to catalytic hydrogenation, in the presence of a catalyst such as platinum, palladium, rhodium or nickel, under a pressure between 1 and 30 bar, to drive, after the eventual deprotection or reprotection of the acid function, to the compound of F FORMULA (I).