| 摘要 |
NEW MATERIAL:A proline derivative shown by the formula I (R1 is pentyl, or hexyl; R2 and R4 are the same or different, H, or lower alkyl; R3 is lower aklyl) and its salt. EXAMPLE:N-[ ( R )-1-Ethoxycarbonyl-2-hexylthioethyl ]-alanyl-( S )-proline-t-butyl ester.alpha-isomer. USE:Having improved inhibitory actions on an enzyme capable of converting angiotensin, useful as a hypotensor. Having enhancing action on immunological competence, expectorating action, and lowering action on intraocular pressure, useful as an adjuvant, expectorant, and a remedy for glaucoma. Having long durability of action time, an imediate effect in a short time, having low toxicity. PREPARATION:A compound shown by the formula II is reacted with a compound shown by the formula III (R5 is hydroxyl group, lower alkoxy group, etc.; X is halogen, etc.) in a solvent such as methanol, etc. in the presence of a deoxidizer, to give a compound shown by the formula I. |
