NOVEL AMINO ACID DERIVATIVE

摘要

NEW MATERIAL:An amino acid derivative expressed by formula I (R<1> is carbamoyl or lower alkoxycarbonyl; His is L-histidyl; n is 0 or 1; Y is O or NH; R<2> is 1-7C alkyl) and acid addition salt thereof. EXAMPLE:Isopropyl (2RS,3S)-[3-(methoxycarbonyl)-2-(1-naphthylmethyl)propionyl- L-histidyl]amino-2-hydroxy-5-methylhexanoate. USE:With strong inhibitory action on resin activity and useful as an orally administrable remedy for hypertension with low toxicity. PREPARATION:A compound expressed by formula II is condensed with a compound expressed by formula III (X is acid residue) using diphenylphosphoric acid azide to afford the aimed compound expressed by formula I. The compound expressed by formula II is synthesized from, e.g. 1-naphthaldehyde and diethyl succinate.