抗抑郁症药吗氯贝胺的合成工艺研究  

Study on the synthesis of moclobemide as the anti-depression drug

作　　者：周石洋 陈玲 ZHOU Shiyang;CHEN Ling(College of Chemistry and Chemical Engineering,Hainan Normal University,Haikou,Hainan 571158,China;Key Laboratory of Tropical Medicinal Plant Chemistry of Ministry of Education,Hainan Normal University,Haikou,Hainan 571158,China;Chongqing City,the Second Middle School of Dianjiang,Dianjiang,Chongqing 408318,China)

机构地区：[1]海南师范大学化学与化工学院,海南海口571158 [2]海南师范大学热带药用植物化学教育部重点实验室,海南海口571158 [3]重庆市垫江县第二中学,重庆垫江408318

出　　处：《贵州师范大学学报（自然科学版）》2019年第1期47-52,共6页Journal of Guizhou Normal University：Natural Sciences

基　　金：重庆市创新创业示范团队科技人才专项(No.cstc2018kjrc-sftd0210);海南师范大学研究生创新科研课题(No.HSYX2018-8)

摘　　要：以4-氯苯甲酸为起始原料,经酰胺化、酰氯化和缩合(N-烷基化)三步反应,合成具有抗抑郁症作用的吗氯贝胺。该合成方法具有原料易得、总收率高、对设备要求低和操作简单等优点,具有发展成为适用于工业化大规模生产的潜能。在合成过程中,对每步反应条件进行了优化,在最佳反应条件下总收率达72. 6%。目标产物及中间产物结构都经~1H NMR、^(13)C NMR、MS和元素分析法进行表征。Using 4-chlorobenzoic acid as the raw material,anti-depression effects moclobemide was synthesized by three steps of animation,acylation and condensation(N-alkylation).The synthetic method has the advantages of easy access to raw materials,high total yield,low requirements on equipment and easy operation.And synthetic method has the potential to be developed for large-scale industrial production.In the synthesis process,the reaction conditions of each step were optimized,and the total yield reached 72.6%under the optimal reaction conditions.The structure of target products and intermediate products were characterized by 1H NMR,13 C NMR,MS and elemental analysis.

关 键 词：吗氯贝胺 抑郁症 优化 表征 

分 类 号：O621.3[理学—有机化学] R914.5[理学—化学]