发明名称 GAMMA-OXO-HOMOPHENYLALANINE DERIVATIVE AND PRODUCTION OF HOMOPHENYLALANINE DERIVATIVE BY REDUCING THE SAME
摘要 PROBLEM TO BE SOLVED: To obtain the subject new compound useful as a constituent component for a medicine, mainly an angiotensin converting enzyme inhibitor. SOLUTION: This compound is shown by formula I (X<1> and X<2> are each H, a 1-7C alkyl, a 6-10C aryl, etc.; R is phenyl, naphthyl, etc.) such as (αR,1R)- N-(1-phenethyl)-γ-oxo-p-methoxy-homophenylalanine. The compound can be obtained by subjecting aβ-benzoylacrylic acid derivative of formula II with a 1-arylethylamine derivative of formula III in a blending ratio of about 3:1 to 1:3 to Michael addition reaction at 0-80 deg.C preferably in a protonic solvent. Further the prepared compound of formula I is reduced with a reducing agent (preferably hydrogen or formic acid) in the presence of a metal catalyst (preferably a palladium catalyst) in an alcohol containing a mineral acid to readily give a compound of formula IV.
申请公布号 JPH10287632(A) 申请公布日期 1998.10.27
申请号 JP19970365161 申请日期 1997.12.18
申请人 KANEGAFUCHI CHEM IND CO LTD 发明人 YAMADA MASAHIKO;NAGASHIMA NOBUO;HASEGAWA JUNZO
分类号 B01J23/44;C07B53/00;C07B61/00;C07C227/08;C07C227/18;C07C229/36;C07C253/30;C07C255/58;C07C319/20;C07C323/63;(IPC1-7):C07C229/36 主分类号 B01J23/44
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