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1. 发明申请

WO0009483A3 PROCESS AND INTERMEDIATES FOR PRODUCTION OF DONEPEZIL AND RELATED COMPOUNDS 审中-公开
标题翻译：二苯醚及其相关化合物的生产过程和中间体
公开(公告)号：WO0009483A3
公开(公告)日：2001-06-21
申请号：PCT/IL9900436
申请日：1999-08-11
申请人： FINETECH LTD , GUTMAN L ARIE , SHKOLNIK ELEONORA , TISHIN BORIS , NISNEVICH GENADY , ZALTZMAN IGOR
发明人： GUTMAN L ARIE , SHKOLNIK ELEONORA , TISHIN BORIS , NISNEVICH GENADY , ZALTZMAN IGOR
IPC分类号： C07B53/00 , C07B61/00 , C07D211/32 , C07D211/34
CPC分类号： C07D211/32 , C07D211/34
摘要： The present invention relates to a new process for the preparation of acetylcholinesterase inhibitors of formula (I) or a salt thereof, wherein: R is N-acyl-4-piperidyl; N-alkoxycarbonyl-4-piperidyl; 4-piperidyl; N-alkyl-4-piperidyl; N-benzyl-4-piperidyl; N-( omega -aralkyl)-4-piperidyl; 4-pyridyl; R , R , R and R are identical or different and each represents hydrogen, straight-chain or branched alkyl, aryl, hydroxy, alkoxy, aryloxy, benzyloxy, acyloxy, alkylthio, arylthio, benzylthio, acylamino, phthalimido or halogen; n is 1, 2 or 3; m is 1, 2, 3, 4 or 5. This process comprises cyclisation of a compound of formula (II) or salts thereof, wherein R , R , R , R and R , m and n are as defined above; R is selected from a derivatised or non-derivatised carboxyl, cyano, N-substituted aminocarbonyl groups or hydrogen; R is selected from a derivatised or non-derivatised carboxyl, cyano or N-substituted aminocarbonyl groups, optionally in the presence of acids and/or solvents. One of the most potent acetylcholinesterase inhibitors of the class of compounds prepared according to the present invention is donepezil.
摘要翻译：本发明涉及制备式（I）的乙酰胆碱酯酶抑制剂或其盐的新方法，其中：R 1是N-酰基-4-哌啶基; N-烷氧羰基-4-哌啶基; 4-哌啶基; N-烷基-4-哌啶基; N-苄基-4-哌啶基; N-（ω-芳烷基）-4-哌啶基; 4-吡啶基; R 4，R 5，R 6和R 7相同或不同，各自表示氢，直链或支链烷基，芳基，羟基，烷氧基，芳氧基，苄氧基，酰氧基，烷硫基，芳硫基，苄硫基，酰氨基，苯二甲酰亚氨基或卤素; n为1,2或3; m为1,2,3,4或5.该方法包括式（II）化合物或其盐的环化，其中R 1，R 4，R 5，R 6和R 7，m和n如上所定义; R 2选自衍生或未衍生的羧基，氰基，N-取代的氨基羰基或氢; R 3选自衍生化或非衍生的羧基，氰基或N-取代的氨基羰基，任选在酸和/或溶剂的存在下。根据本发明制备的化合物类别中最有效的乙酰胆碱酯酶抑制剂之一是多奈哌齐。

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