A new industrial process for oxcarbazepine

被引：23

作者：

Fuenfschilling, PC ^{[1
]}

Zaugg, W ^{[1
]}

Beutler, U ^{[1
]}

Kaufmann, D ^{[1
]}

Lohse, O ^{[1
]}

Mutz, JP ^{[1
]}

Onken, U ^{[1
]}

Reber, JL ^{[1
]}

Shenton, D ^{[1
]}

机构：

[1] Novartis Pharma AG, CH-4002 Basel, Switzerland

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2005年 / 9卷 / 03期

关键词：

D O I：

10.1021/op049760a

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

A novel industrial process for the antiepileptic drug oxcarbazepine I has been developed. Unlike the old process, the new process is free from halogenated solvents and can be performed in standard production equipment. It starts from commercially available 1,3-dihydro-1-phenyl-2H-indol-2-one 10. In the key step, an electrophilic ring closure reaction of 2-[(methoxycarbonyl)phenylamino] benzeneacetic acid 5 to 10,11-dihydro-10-oxo-5H-dibenz[b,f]azepine-5-carboxylic acid methyl ester 6 in poly phosphoric acid was applied. For the manufacture of 5, a highly efficient process using a dianion strategy was developed.

引用

页码：272 / 277

页数：6