发明名称 PRODUCTION OF SUBSTITUTED PIPERIDINE EPOXIDE
摘要 PROBLEM TO BE SOLVED: To produce a substituted piperidine epoxide useful for efficiently synthesizing a renin inhibitor by epoxidizing a specific compound. SOLUTION: By epoxidizing a compound of formula I [A is arylene; R1 is CR3R4R5 (R3 is H; R4 is an aryl; R5 is an alkyl, an aryl or the like; C* is asymmetric carbon atom); R2 is an O-alkyl, an O-cycloalkyl, an O-aryl or the like] or its salt a compound of formula II is obtained. The compound of formula I is e.g. (1R,6R)-6-(4-benzyloxy-phenyl)-3-[(R)-1-phenyl-ethyl]-7-oxa-3-aza- bicyclo[4.1.0]heptane or the like. The compound of formula II is a new substance and is e.g. (3R,4S,5S)-4-[4-(3-benzyloxy-propoxy)-phenyl]-5- ethoxy-3-(naphthalen-2-ylmethoxy)-piperidine.
申请公布号 JP2000063383(A) 申请公布日期 2000.02.29
申请号 JP19990226173 申请日期 1999.08.10
申请人 F HOFFMANN LA ROCHE AG 发明人 GUELLER ROLF;LOHRI BRUNO;SCHMID RUDOLF
分类号 C07D211/52;C07D211/70;C07D211/74;C07D491/04;C07D491/044;C07D491/08;(IPC1-7):C07D491/044 主分类号 C07D211/52
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