| 摘要 |
NEW MATERIAL:A compound expressed by formula I [R<1> is 1-3C monoalkylamino, 2-6C dialkylamino or cyclic amino expressed by formula II (Y is single bond, -O- or -CH2-); His is L-histidyl; n is 0 or 1; X is -O- or -NH-; R<2> is 1-7C alkyl] and a pharmacologically acceptable acid addition salt thereof. EXAMPLE:Isopropyl (2RS, 3S)-3-{N-[2-(1-naphthylmethyl)-3-(morpholinocarbonyl) propionyl]-L-histidyl}amino-2-hydroxy-5-methylhexanoate. USE:A medicine, having powerful inhibitory action on renin and useful as an orally administrable remedy for hypertension with low toxicity. PREPARATION:A compound expressed by formula III (formula IVis L- configuration) is suspended in N,N-dimethylformamide, and hydrogen chloride is added thereto. Isoamyl nitrite and further triethylamine are added thereto and reacted with a compound expressed by formula V to afford the aimed compound expressed by formula I.
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