摘要 |
Captopril (1-[(2S)-3-mercapto-2-methylpropionyl]-L-proline) of formula (I) is prepared from 2-methyl-1,3-propandiol by microbial oxidation to obtain (R)-3-hydroxy-2-methyl propionic acid, by chlorination to obtain (R)-3-chloro-2-methyl propionyl chloride and by subsequent reaction with L-proline to obtain the corresponding N-(3-chloro-2-methylpropionyl-L-proline) and by conversion of the chloromethyl group into the mercaptomethyl group. Captopril is a antihypertensive pharmaceutical active substance. |