公开(公告)号：US4069230A

公开(公告)日：1978-01-17

申请号：US691777

申请日：1976-06-01

申请人： Shigeaki Morooka ,  Katsumi Tamoto ,  Akira Matuura

发明人： Shigeaki Morooka ,  Katsumi Tamoto ,  Akira Matuura

IPC分类号： C07D209/40 ,  C07D209/04 ,  C07D491/056

CPC分类号： C07D209/04

摘要： An improved process for preparing indole derivatives of the formula, ##STR1## wherein R.sub.1 and R.sub.2 each are hydrogen, halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, nitro, cyano or trifluoromethyl, or when taken together, form methylenedioxy; R.sub.3 is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, nitro, cyano or dimethylamino; and R.sub.4 is hydrogen or halogen, which comprises cyclizing a compound of the formula, ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined above, with an acidic condensing agent.The indole derivatives of the formula (I) mentioned above are useful as a key intermediate for the preparation of benzodiazepines, which are useful as tranquilizers, muscle relaxants and the like.

摘要翻译： 制备下式的吲哚衍生物的改进方法：其中R 1和R 2各自为氢，卤素，C 1 -C 3烷基，C 1 -C 3烷氧基，硝基，氰基或三氟甲基，或当一起形成亚甲二氧基 ; R3是氢，卤素，C1-C3烷基，C1-C3烷氧基，硝基，氰基或二甲基氨基; 并且R 4是氢或卤素，其包括使式III化合物，其中R 1，R 2，R 3和R 4如上所定义的化合物与酸性缩合剂环化。