盐酸西布曲明的合成工艺改进

目的研究盐酸西布曲明适合工业化大生产的方法。方法以对氯氯苄为原料,经取代、环合、加成、还原、二甲基化及成盐等反应合成盐酸西布曲明,并对反应条件进行了改进和优化。结论工艺经改进和优化后,反应条件温和,操作简便,工艺稳定,总收率达到57.8%,大幅度的降低了生产成本,更加适合工业化生产。

Improvoed synthesis of sibutramine hydrochloride

OBJECTIVE To study the synthesis of sibutramine hydrochloride method which is suit for industrial production.METHODS Sibutramine hydrochloride was synthesized from the material 4-chlorobenzyl chloride by substibution,cyclization,addition,reduction,dimethylation to afford sibutramine which followed by salt formation with hydrochloride,and the reaction condition werd improved and optimized.CONCLUSION This improved and optimized synthesis has more advantages such as mild reaction condition,simple operation,stable process,high total yield which is 57.8%;And this synthetic technique reduces production costs substantially which is more suitable for industrial production.