NOVEL METHOD FOR SYNTHESIS OF N-(S)-1-CARBOXYBUTYL-(S)-ALANINE ESTERS AND USE IN SYNTHESIS OF PERINDOPRIL

摘要

The stereoselective and industrial scale process of the present invention provides compounds of formula (I) wherein R is straight or branched C 1-6 alkyl. The compound is used in the preparation of perindopril and its pharmaceutically acceptable salts. In the process, the sodium pyrurate of the formula (III) is condensed with a compound of the formula (IV) during palladium-catalyzed hydrogenation in water in the presence of one mole of 0.1 to 0.2 moles of the compound of the formula (IV) calculated as sodium hydroxide. SHE