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A New Industrial Process for 10-Methoxyiminostilbene: Key Intermediate for the Synthesis of Oxcarbazepine
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2009-08-20 00:00:00 , DOI: 10.1021/op900127v
Harnam Singh 1 , Nitin Gupta 1 , Pramod Kumar 1 , Sushil K. Dubey 1 , Pawan K. Sharma 1
Affiliation  

A new industrial process, involving only two isolation and drying steps, for 10-methoxyiminostilbene (MISB), an advance intermediate of widely prescribed antiepileptic drug, oxcarbazepine, has been developed. A salient feature of this process is the novel use of 1,3-dibromo-5,5-dimethylhydantoin (DBDMH) to afford bromohydrin methyl ether from N-acetyliminostilbene. The byproducts of this process namely acetic acid, 5,5-dimethylhydantoin and Et3N·HBr are recyclable as well as nontoxic. This process is amenable for the large-scale production of MISB.

中文翻译:

10-甲氧基亚氨基二苯乙烯的新工业工艺:合成奥卡西平的关键中间体

已开发出一种新的工业工艺,仅涉及两个分离和干燥步骤,即10-甲氧基亚氨基二苯乙烯(MISB),这是广泛使用的抗癫痫药奥卡西平的高级中间体。该方法的显着特征是新颖地使用1,3-二溴-5,5-二甲基乙内酰脲(DBDMH)从N-乙酰基亚氨基二苯乙烯制得溴代醇甲基醚。该方法的副产物,即乙酸,5,5-二甲基乙内酰脲和Et 3 N·HBr可回收且无毒。该工艺适合于MISB的大规模生产。
更新日期:2009-08-20
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