NOVEL PROLINAL DERIVATIVE, PRODUCTION THEREOF AND ANTIAMNESIC AGENT CONTAINING SAID DERIVATIVE

摘要

NEW MATERIAL:A compound expressed by formula I [A is formula II (either of R1 and R2 is H and the other is 2-5C alkyl, 1-5C alkoxy, phenyl, etc., or formula III (m is 3-6); n is 3-10; D is halogen, nitro or carbocyclic ring unsubstituted or substituted by a 1-4C alkyl]. EXAMPLE:N-(2-Isopropyl-6-phenylhexanoyl)-L-prolinal. USE:An antiamnesic agent having inhibitory activity against prolyl endopeptidase. PREPARATION:A prolinol derivative expressed by formula IV is subjected to oxidative reaction using a tertiary amine or oxidizing agent (e.g. sulfur trioxide-pyridine complex) in a solvent, such as DMSO, at 0-50 deg.C to afford the aimed compound expressed by formula I.