1-(3'-(Rhodanido)-2'-(methyl)-propionyl)-pyrrolidine-2-carboxylic acid - which is intermediate for antihypertensive agent 1-(3'-mercapto)-(2's)-(methyl)-propionyl)- pyrrolidine-(2s)-carboxylic acid

摘要

1-(3'-rhodanido)-2'-(methyl)-propionyl)-pyrrolidine-2- carboxylic acid of formula (I) is new. USE/ADVANTAGE - (I) (Esp. the 2s, 2's-enantiomer) is an intermediate in the prepn. of 1-(3'-(mercapto)-(2's)- (methyl)-propionyl)-pyrrolidine I -(2s)-carboxylic acid (captopril) which can be used to reduce blood pressure. The prepn. of captopril from L-proline via (I) gives yields of more than 50% (based on L-proline, compared to e.g. a previous process using 3-(ethanoylthio)-2-(methyl)-propionic acid as the acylating agent, which gave yields of only 10% based on L-proline. Other previous processes, were little better, giving yields of 30% or 34-35%. The prepn. via (I) is simple. (I) itself is produced by a simple and economical process.