马来酸氟伏沙明-D3的合成  

Synthesis of Fluvoxamine Maleate-D3

作　　者：仇中选 王东[1] 黄龙江[2] QIU Zhongxuan;WANG Dong;HUANG Longjiang(School of Biological&Chemical Engineering,Qingdao Technical College,Qingdao 266555,China;College of Chemical Engineering,Qingdao University of Science and Technology,Qingdao 266042,China)

机构地区：[1]青岛职业技术学院生物与化工学院,山东青岛266555 [2]青岛科技大学化工学院,山东青岛266042

出　　处：《合成化学》2022年第9期726-732,共7页Chinese Journal of Synthetic Chemistry

基　　金：山东省自然科学基金资助项目(ZR2020MB104)。

摘　　要：以4-苄氧基-1-丁醇(2)为起始原料,氘代碘甲烷为氘代试剂,经氘代甲基化、氢化脱苄、溴化、格氏反应、戴斯-马丁氧化、缩合、取代和成盐等反应,以51.7%总收率合成了稳定同位素标记的马来酸氟伏沙明-D_(3)(1)。该合成方法原料易得、操作简单、重现性好。目标化合物的结构经核磁共振和高分辨质谱确认,可用于药代动力学研究。With 4-benzyloxy-1-butanol(2) and isotope labeling iodomethane as precursors,the stable fluvoxamine maleate-D(1) was synthesized via methylation,debenzylation,bromination reaction,Grignard reaction,Dess-Martin oxidation,nucleophilic addition,substitution and salt forming reaction.Based on the consumption of iodomethane-D_(3),the yield of fluvoxamine maleate-Dwas 51.7% and the structure was confirmed by HRMS,^(1)H NMR and ^(13)C NMR.Fluvoxamine maleate-Dcould be used as the internal standard reagent in pharmacokinetics.The synthetic method has the advantages of low cost of starting materials,facile operation process and good reproducibility.

关 键 词：同位素标记 马来酸氟伏沙明-D3 碘甲烷-D3 合成 甲基化 戴斯-马丁氧化 

分 类 号：O628[理学—有机化学]