盐酸维拉唑酮的合成方法改进  

Improved method for synthesis of vilazodone hydrochloride

作　　者：程青芳[1,2] 王启发[1] 邱峰[2] 唐建平[2] 廖云鹏[2] 

机构地区：[1]江苏省海洋资源开发研究院,连云港222001 [2]淮海工学院化工学院,连云港222005

出　　处：《中国新药杂志》2013年第2期226-229,共4页Chinese Journal of New Drugs

基　　金：江苏省"六大人才高峰"高层次人才项目;连云港市工业攻关项目(CG1106);江苏省海洋生物技术重点建设实验室基金资助项目(2009HS04)

摘　　要：目的:改进盐酸维拉唑酮的合成工艺。方法:以5-溴水杨醛和溴代丙二酸二乙酯为原料,经醚化、环合、酰胺化、取代、水解制得中间体5-(1-哌嗪基)苯并呋喃-2-甲酰胺(7)。7再与3-(4-氯丁基)-1H-5-氰基吲哚(11)经取代和与盐酸成盐制得盐酸维拉唑酮。其中,11是用5-氰基吲哚和4-氯丁酰氯经酰化、还原得到的。结果:工艺的总收率为39.1%;盐酸维拉唑酮的结构经质谱、核磁共振谱确证。结论:该方法工艺简单,收率高,适合工业化生产。Objective： To improve the synthesis of vilazodone hydrochloride. Methods： The important in- termediate 5-（1-piperazinyl） benzofuran-2-carboxamide （7） was prepared from 5-bromosalicylaldehyde and diethyl bromomalonate by etherification synthesized from 7 and 3-（4-c cyclization, amidation, substitution and hydrosis. Vilazodone hydrochloride was orobutyryl）-lH-indole-5-carbonitrile （11） by substitution and salification with hydrochloride. The important intermediate 11 was prepared from 5-cyanoindole and 4-chlorobutyric acid chloride by acylation and reduction. Results： The total yield was 39.1% The structure of vilazodone hydrochloride was identi- fled by MS and 1H-NMR. Conclusion： This improved method is simple, high yield and suitable for industrial pro- duction.

关 键 词：盐酸维拉唑酮 抗抑郁 合成 

分 类 号：R914.5[医药卫生—药物化学]