卡马西平无溴合成工艺

A Bromide-free Process for Carbamazepine

以邻硝基甲苯和邻氯苯甲醛为起始原料,经醇醛缩合、脱水、还原、环合得关键中间体亚氨基芪,再与三光气酰氯化、氨化得卡马西平,总收率31%。起始原料价廉易得,合成路线短,不涉及溴化物,有望成为工业化路线。

The key intermediate iminostilbene was synthesized from 2-nitrotoluene and 2-chlorobenzaldehyde via aldol condensation, dehydration, reduction and cyclization, which was subjected to acyl chlorination with bis（trichloromethyl）- carbonate and ammonifi cation with ammonia to give the target product carbamazepine with an overall yield of about 31%. This bromide-free process had the advantage of inexpensive materials and short reaction steps, it was suitable for large-scale production.