申请人:Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.
公开号:US04395549A1
公开(公告)日:1983-07-26
Intermediates useful in the preparation of Rutecarpine and Rutecarpine derivatives are disclosed as well as a process for the preparation of said intermediates having the following formula: ##STR1## wherein R, R.sup.1 and R.sup.2 are the same or different and stand for hydrogen, halogen, nitro, carboxy, nitrile, alkoxy containing 1 to 4 carbon atoms, alkoxycarbonyl containing 1 to 4 carbon atoms in the alkoxy group, alkyl containing 1 to 4 carbon atoms, amino or hydroxy or R and R.sup.1 together stand for methylenedioxy, R.sup.2 stands for hydrogen, R.sup.3 represents hydrogen or alkyl containing 1 to 4 carbon atoms, R.sup.4 stands for phenyl, phenyl substituted by 1 to 3 same or different substituents selected from the group of halogen(s), alkyl, and alkoxy containing 1 to 4 carbon atoms, phenyloxy, hydroxy, nitro, amino, cyano, carboxy, alkoxycarbonyl having 1 to 4 carbon atoms, alkanoyl having 1 to 4 carbon atoms, methylenedioxy, trifluoromethyl, phenyl and dialkylamino having 1 to 4 carbon atoms in the alkyl part or naphthyl and the dotted line indicated an optional double bond. Also pharmaceutically acceptable acid addition and quaternary ammonium salts are disclosed.
本文公开了在Rutecarpine和Rutecarpine衍生物制备中有用的中间体,以及制备该中间体的过程,该中间体具有以下结构式:##STR1## 其中R,R.sup.1和R.sup.2相同或不同,代表氢,卤素,硝基,羧基,腈基,含1至4个碳原子的烷氧基,烷氧羰基,在烷氧基中含有1至4个碳原子的烷基,氨基或羟基,或者R和R.sup.1一起代表亚甲二氧基,R.sup.2代表氢,R.sup.3代表氢或含1至4个碳原子的烷基,R.sup.4代表苯基,苯基被1至3个相同或不同的卤素、烷基和在烷氧基中含有1至4个碳原子、苯氧基、羟基、硝基、氨基、腈基、羧基、含有1至4个碳原子的烷氧羰基、含有1至4个碳原子的脂肪酰基、亚甲二氧基、三氟甲基、苯基和在烷基部分含有1至4个碳原子的二烷基氨基取代的苯基取代,或者萘基,虚线表示可选的双键。此外,还公开了药学上可接受的酸添加物和季铵盐。