摘要
目的:探讨盐酸舍曲林合成工艺。方法:以1-萘酚与邻二氯苯为原料,经过Friedel-Crafts烷基化反应,制备重要的中间体4-(3,4-二氯苯基)-1-萘满酮。然后通过甲胺席夫碱的Raney-Ni催化还原反应,成盐得到顺式消旋盐酸舍曲林。经D-(-)-扁桃酸拆分后成盐得到顺-(+)-盐酸舍曲林。结果与结论:该合成工艺所得产品顺-(+)-盐酸舍曲林比旋光值[α]D20=+38.3(c=2.0甲醇),总收率达到26%。该合成工艺操作简单,原料易得,条件温和,适合工业化生产。
Aim： To optimize the synthesis of sertraline hydrochloride. Methods：The intermediate 4-（3,4-dichloro- phenyl）-1-tetralone was prepared by Fridel-Crafts alkylation of alpha-naphthol with orthodichlorobenzene. The cis-（ ＋ ）ser- traline hydrochloride was obtained by hydrogenating the shift base of methylamine using Raney-Ni as catalyst, then reacting with HCl. The cis-（ ＋ ）-sertraline was resolved by D-（ - ）-mandlic acid. Results and conclusion： The total yield of the optimized process is 26% and the optical rotation of cis-（ ＋ ）-sertraline is ＋ 38. 3 （ c = 2, methanol）. The optimized process is valuable for industrial production.
出处
《郑州大学学报（医学版）》
CAS
北大核心
2008年第4期785-787,共3页
Journal of Zhengzhou University(Medical Sciences)
关键词
盐酸舍曲林
抗抑郁
合成
sertraline hydroehloride
antidepressant
synthesis
