抗高血压药物维拉帕米的合成  

Synthesis of Antihypertensive Drug Verapamil

作　　者：李旻玥 宋荣聪 任杰[1] 胡昆[1] LI Min-yue;SONG Rong-cong;REN Jie;HU Kun(School of Pharmacy, Changzhou University, Changzhou 213164, China)

机构地区：[1]常州大学药学院,江苏常州213164

出　　处：《合成化学》2021年第12期1077-1082,共6页Chinese Journal of Synthetic Chemistry

基　　金：江苏省研究生科研与实践创新计划项目(SJCX19_0633)。

摘　　要：以3,4-二甲氧基苯乙酸为原料,经酰化、脱水、C-烷烃化反应、得到关键中间体α-异丙基-3,4-二甲氧基苯乙腈(5);再以3,4-二甲氧基苯乙酸为原料,经酰化、还原、N-烷烃化反应得到N-(γ-氯丙基)-N-甲基-3,4-二甲氧基苯乙胺(2);2与5经过缩合得到了最终产物维拉帕米,总收率为25.4%,其结构经^(1)H NMR和^(13)C NMR确证。该合成路线具有原料廉价易得、操作简便、反应条件温和、后处理简便、收率较好等优点,具有较高的工业化前景。Using 3,4-dimethoxyphenylacetic acid as the raw material,the key intermediateα-isopropyl-3,4-dimethoxybenzeneacetonitrile(5)is obtained through acylation,dehydration,and C-alkanization reaction;3,4-Dimethoxyphenylacetic acid is used as the raw material,and N-(γ-chloropropyl)-N-methyl-3,4-dimethoxybenzene ethyl is obtained through acylation,reduction,and N-alkanization.Amine(2)and 5 were condensed to obtain the final product Verapamil with a total yield of 25.4%.Its structure was confirmed by ^(1)H NMR and ^(13)C NMR.This synthetic route has the advantages of cheap and easy-to-obtain raw materials,simple operation,mild reaction conditions,simple post-processing,good yield,and has a high industrial production prospect.

关 键 词：高血压药 3 4-二甲氧基苯乙酸 缩合 维拉帕米 合成 

分 类 号：O626[理学—有机化学]