发明名称 |
NEW PIRROLO 3,2-e]INDOL DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND APPLICATIONS. |
摘要 |
<p>The new pirrolo [3,2-e]indol derivatives have the formulae (I), (Ia) and (II) wherein R is substituted or unsubstituted aryl or heteroaryl, R' is substituted or unsubstituted alcanoyl, alkenoyl, alkinoyl, arenocarbonyl or heterareocarbonyl and X is chloro, bromo, iodo or alkylsulfonyl or arylsulfonyl. The process comprises: (a) deacylating (VII) in order to obtain (VIII); (b) subjecting (VIII) to a cyclopropyl ring opening raction in order to give (IX); (c) reacting (IX) with acid R-COOH in order to yield (I); (d) optionally, reacting (I) with a base in the presence of a condensing agent in order to obtain (II); (e) optionally, reacting (I) with a carboxylic acid in the presence of a condensing agent or with an acid chloride in the presence of a base to give (Ia). The compounds (I), (Ia) and (II) find application as agents having antitimoral activity for the treatment of cancer. <CHEM></p> |
申请公布号 |
EP0680964(A1) |
申请公布日期 |
1995.11.08 |
申请号 |
EP19950900773 |
申请日期 |
1994.11.18 |
申请人 |
UNIVERSIDAD DE SANTIAGO DE COMPOSTELA |
发明人 |
DELAMANO GARCIA, JOSE;TOJO SUAREZ, GABRIEL;LOPEZ GOTI, CARMEN;FERNANDEZ ALMEIDA, JESUS;GARCIA GRAVALOS, DOLORES;FAIRCLOTH, GLYNN THOMAS |
分类号 |
A61K31/40;A61P35/00;C07D487/04;C07D487/10;(IPC1-7):C07D487/04 |
主分类号 |
A61K31/40 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|