2-(Methyl)-3-(rhodanido)-propionic acid - which is intermediate for antihypertensive agent 1-(3'-(mercapto)-(2's)-pyrrolidine-(2s)-carboxylic acid

2-(methyl)-3-(rhodanido)-propionic acid of formula (I) is new. USE/ADVANTAGE - (i) (Esp. the S-enantiomer) is an intermediate in the prepn. of 1-(3'-(mercapto)-(2's)- (methyl)-propionyl)pyrrolidine-(2s)-carboxylic acid (captopril) which can be used to reduce blood pressure. The prepn. of c...

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Main Authors DIETZ, ANDRAS, UERMOES, GEB. LASSU, GABRIELLA, JAKFALVI, ELEMER, KOVACS, GEB. PALOTAI, AGNES, BLASKO, GABOR, SCHNEIDER, GEZA, SZTRUHAR, ILONA., BUDAPEST, HU, BECK, IVAN
Format Patent
LanguageEnglish
German
Published 26.03.1992
Subjects
ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:2-(methyl)-3-(rhodanido)-propionic acid of formula (I) is new. USE/ADVANTAGE - (i) (Esp. the S-enantiomer) is an intermediate in the prepn. of 1-(3'-(mercapto)-(2's)- (methyl)-propionyl)pyrrolidine-(2s)-carboxylic acid (captopril) which can be used to reduce blood pressure. The prepn. of captopril from L-proline using (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 acylating agent, which gave yields of only 10% (based on L-proline) other processes were little better, giving yields of 30% or 34-35%. The prepn. using (I) is simple. (I) is itself produced by a simple and economical process.
Bibliography:Application Number: DE19914123214