| 摘要 |
<p>NEW MATERIAL:A compound expressed by formula I (R1 represents H or protecting group of the carboxyl group; R2 and R3 each represent H or lower alkyl; R4 represents lower alkyl, cycloalkyl, aryl, etc.; A represents OH, mercapto, acylthio, carboxyl, etc.). EXAMPLE:Bis-[methyl N-(2-thiobenzoyl)L-prolinate]disulfide. USE:A hypotensor having inhibitory action on angiotensin converting enzymes. PREPARATION:A carboxylic acid expressed by formula II or its reactive derivative is reacted with a compound expressed by formula III to obtain a compound expressed by formula IV, which is then reduced in the presence of a reducing agent such as triphenylphosphine under acidic conditions within room temperature -50 deg.C range. Further, if necessary, hydrolysis of the protecting group of the carboxyl group or acylation of the mercapto group is carried out to obtain the compound expressed by formula I (A represents mercapto or acylthio).</p> |
