发明名称 Bicyclo{8 3.1.0{9 hexylethylaminocarbonyl-substituted naphthyloxy cardiovascular agents
摘要 1-Alkylamino-3-([2-(endobicyclo[3.1.0]-hex-6-yl)ethylaminocarbonyl]nap hthyloxy)-2-propanols and methods for preparing these compounds are disclosed. The compounds are useful in the treatment of hypertension and abnormal heart conditions in mammals. These compounds are prepared by the treatment of the corresponding 1,2-epoxy-3-[2-(endobicyclo[3.1.0]hex-6-yl)ethylaminocarbonyl]naphthyl oxy)-propane with an alkylamine having the desired alkyl substituent or by base or acid hydrolysis of the corresponding 2-optionally substituted -3-alkyl-5-([2-(endobicyclo[3.1.0]hex-6-yl)ethylaminocarbonyl]naphthyl oxymethyl)oxazolidine. These latter compounds can be prepared by condensing a hydroxy-substituted naphthalene with a 3-alkyl-5-tosyloxymethyloxazolidine such substituted or unsubstituted at the 2-position or alternatively, by treating the former aminopropanol compounds of the present invention with an aldehyde having the desired substituent. These latter oxazolidine compounds are also active for treatment of hypertension and abnormal heart conditions.
申请公布号 US4145443(A) 申请公布日期 1979.03.20
申请号 US19770846952 申请日期 1977.10.31
申请人 SYNTEX (U.S.A.) INC. 发明人 UNTCH, KARL G.;UNGER, STEFAN H.
分类号 C07C29/14;C07C29/17;C07D263/06;C07D303/22;(IPC1-7):C07C103/29 主分类号 C07C29/14
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