绿卡色林盐酸盐的合成方法

Synthetic Methods of Lorcaserin Hydrochloride

绿卡色林盐酸盐,化学名称为(R)-8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并氮杂卓盐酸盐,是一种作用于中枢神经系统的新型减肥药,自上市以来受到了极大的关注。本文依据国内外文献,分别以4-氯苯乙胺、4-氯苯乙酸/酯和4-氯苯乙醇为原料,综述了绿卡色林外消旋体的合成路线并简述了每条路线的优缺点,最后介绍了拆分外消旋体得到绿卡色林的方法。

Lorcaserin hydrochloride （ （R） - 8 - Chloro - 1 - methyl - 2,3,4,5 - tetrahydro - 1 H - 3 - benzazepine hydrochloride） was a new type of diet medicine in the role of the central nervous system and was paid a great deal of attention since being listed. Based on literatures, synthetic methods of Lorcaserin racemic were reviewed via 4 - chlorophenethylamine, 4 - chlorophenylacetie acid/ester or 4 - chlorophenylethanol as raw materials and the advantages or disadvantages of each method were briefly discussed. Finally, the configuration separation method was introduced and Lorcaserin was obtained via this method.