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目的 :改进肥胖症治疗药盐酸西布曲明 (sibutraminehydrochloride)的合成方法。方法 :以 4 氯苄腈为起始原料 ,经环烃化、Grignard反应、还原、Eschweiler clarke甲基化和成盐等反应合成了盐酸西布曲明。结果 :合成产物经熔点、元素分析、红外光谱和核磁共振谱等确证 ,总收率 36.3%。结论 :此合成工艺简便 ,易于工业化生产。
OBJECTIVE: To improve the synthesis of sibutramine hydrochloride, an obesity therapeutic drug. Methods: Sibutramine hydrochloride was synthesized from 4-chlorobenzonitrile as the starting material through cyclic alkylation, Grignard reaction, reduction, methylation of Eschweiler clarke and salt formation. Results: The synthesized product was confirmed by melting point, elemental analysis, IR and 1H NMR. The total yield was 36.3%. Conclusion: This synthetic process is simple and easy to industrial production.