Patent ID: 7157485
Filing Date: 2007-01-02
Classification: A61P,C07D,C07K,Y02P

Abstract:
1. A process for the synthesis of compounds of formula (I): wherein R wherein 1-(1-cyclohexen-1-yl)-pyrrolidine of formula (III): is reacted with a serine compound of formula (IV): wherein R to yield a compound of formula (V): the amine function of the compound of formula (V) is deprotected and the deprotected intermidiate thus obtained is subjected to dehydration, to yield a compound of formula (VI): which is reacted with an alanine compound of formula (VII): wherein R in an organic solvent, in the presence of an amount of dicyclohexylcarbodiimide of from 1 to 1.2 mol per mol of compound of formula (V) used and an amount of triethylamine of from 1 to 1.2 mol per mol of compound of formula (V) used and optionally in the presence of 1-hydroxybenzotriazole, at a temperature of from 20 to 50° C., to yield, after isolation and recrystallisation, a compound of formula (VIII): which is hydrogenated in the presence of a catalyst, under a hydrogen pressure of from 1 to 30 bars, to yield, after optional deprotection or reprotection of the acid function, the compound of formula (I).