| 摘要 |
NEW MATERIAL:The compound of formula I (R1 is 5-14C alkyl, 2-6C alkenyl, etc.; R2 is H or 1-6C alkyl; R3 is 1-6C alkyl; R4 is H, phenyl 1-6C alkyl, etc.; n is 0, 1 or 2) and its salt. EXAMPLE:N-[(R)-1-ethoxycarbonyl-2-hexylthioethyl]-alanyl-(S)-proline beta-isomer. USE:A hypotensor, an immunoactivating agent, a remedy for glaucoma, etc. It has excellent angiotensinase inhibiting activity, rapid activity, long duration time, an low toxicity. PREPARATION:The objective compound can be produced e.g. by reacting the cysteine derivative of formula II with the alpha-keto acid in the presence of a metal hydride complex compound such as lithium borohydride, and reacting the resultant carboxylic acid of formula IV with the amine of formula V in the presence of a condensation agent such as N,N'-dicyclohexylcarbodiimide in a solvent such as THF, at -10 deg.C - room temperature for 3-24hr. |
