氟伏沙明合成方法的改进  

Improvement of synthetic method of fluvoxamine

作　　者：郑滔 汪华 钟旭斌 陈鹏 ZHENG Tao;WANG Hua;ZHONG Xubin;CHEN Peng(Livzon Syntpharm Co.,Ltd.(Zhuhai FTZ),Zhuhai Guangdong 519030)

机构地区：[1]珠海保税区丽珠合成制药有限公司,广东珠海519030

出　　处：《天津化工》2023年第6期44-48,共5页Tianjin Chemical Industry

摘　　要：本文通过对两种合成氟伏沙明的方法进行研究,总结了其在实际合成过程中存在的问题。由于现今合成氟伏沙明的方法的产率较低,且存在许多副产物,加大了产品的提纯难度。因此,本文设计了一系列的保护基团,对关键性原料进行基团保护,最后进行脱保护,以此提高2-氯乙烷胺的利用率。同时,我们对合成N-(2-(((5-甲氧基-1-(4-(三氟甲基)苯基)亚戊基)氨基)氧基)乙基)苯甲酰胺的条件进行了优化,提高了这个过程的产率。最终,氟伏沙明的产率可达90%以上。In this paper,two methods for synthesizing fluvoxamine are introduced,and the problems existing in the actual synthesis process are summarized respectively.Due to the low yield of the current method for synthesizing fluvoxamine,there are many by-products,which increases the difficulty of product purification.Therefore,a series of protective groups were designed in this paper to protect the key raw materials,and finally a deprotection process was carried out to improve the utilization rate of 2-chloroethan-1-amine.Meanwhile,our conditions for the synthesis of N-(2-(((5-methoxy-1-(4-(trifluoromethyl)phenyl)pentylidene)amino)oxy)ethyl)be-zamide optimizations were made to increase the yield of this step.The final yield of fluvoxamine can reach more than 90%.

关 键 词：氟伏沙明 苯甲酸 保护基 优化 

分 类 号：TQ460.1[化学工程—制药化工]