第 45 卷第 1 期 | | Vol. 45 No. 1 | 2015 年 2 月 | Feb 2015 |
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所属栏目:医药及中间体
普瑞巴林的合成及(S)-(+)-3-氨甲酰甲基-5-甲基己酸的消旋 |
孟文学,龙道兵
(重庆朗天制药有限公司,重庆 401221) |
摘 要:(±)-3-氨甲酰甲基-5-甲基己酸经拆分得到(R)-(-)-3-氨甲酰甲基-5-甲基己酸,再经Hofmann降解得到普瑞巴林。提供了(S)-(+)-3-氨甲酰甲基-5-甲基己酸的一种外消旋方法,外消旋体可以作为原料继续套用,提高了原料利用率,降低了成本,有较高的应用价值,具有工业化应用前景。 |
关键词:普瑞巴林;对映异构体;消旋;循环利用 |
中图分类号:TQ463+.2 文献标识码:A 文章编号:1009-9212(2015)01-0042-05 |
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Synthesis of Pregabalin and Racemize of (S)-(+)-3-Carbamoylmethyl-5-methylhexanoic Acid |
MENG Wen-xue, LONG Dao-bing
(Chongqing Landtower Pharmaceutical Co., Ltd., Chongqing 401221, China) |
Abstract:Pregabalin was obtained using(±)-3-carbamoylmethyl-5-methylhexanoic acid as the starting material by a two-step reaction including the racemic resolution and Hofmann degradation. A racemic method was also provided for(S)-(+)-3-carbamoylmethyl-5-methylhexanoic acid in this paper. The racemate could be reused as raw materials leading to lower raw material consumption, higher yield and lower cost for the production of Pregabalin. In addition, this novel method was environmentally friendly, suitable for industrial production with higher application value. |
Key words:Pregabalin; enantiomer; racemize; recycling |
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作者简介:孟文学(1970-),男,重庆渝北人,主要从事药物合成研究(E-mail:mengwx315@163.com)。
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收稿日期:2014-11-2
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