| 摘要 |
PURPOSE:To obtain a new subject derivative consisting of a peptic alcohol derivative containing cyclohexyl group, having strong renin inhibiting activity, exhibiting continuous depressing action by oral administration and useful as a therapeutic agent for hypertension, therapeutic agent for heart failure, etc. CONSTITUTION:An aminoalcohol compound of formula I [R<4> is (substituted)lower alkyl, (substituted)benzyl, etc.; R<5> is lower alkyl] [e.g. (2S,3S,5S)-2-amino-1- cyclohexyl-5-methoxymethoxy-6-methyl-3-heptanol, etc.] is made to react with a N-substituted amino acid, etc., of formula II {A is formula III [W is formula IV (R<10> to R<12> are H, lower alkyl, halogen, etc.; Z<1> is CH2, O, S, SO, SO2, etc.; Z<2> is substituted N, O, substituted methylene, etc.; m and n are 0-5), etc.; X is CO or SO2; Y is CH2, O, etc.; R<1> is (substituted)aralkyl], etc.; R<2> is H or lower alkyl; R<3> is (CH2)dSR<26> [d is 1-5; R<26> is H or lower alkyl]} in the presence of a condensing agent to provide the objective alcohol derivative of formula V. |
