有机化学 ›› 2017, Vol. 37 ›› Issue (2): 503-507.DOI: 10.6023/cjoc201612005 上一篇    下一篇

研究简报

盐酸黄连素的汇聚式合成研究

陈程a, 徐蒙蒙a, 赵青b, 刘承秀c, 杨鸿均a, 冯豫川a   

  1. a 西南民族大学化学与环境保护工程学院 成都 610041;
    b 西南民族大学预科教育学院 成都 610041;
    c 西南民族大学校医院 成都 610041
  • 收稿日期:2016-12-02 修回日期:2017-01-01 发布日期:2017-01-17
  • 通讯作者: 杨鸿均, 冯豫川 E-mail:yanghj@swun.cn
  • 基金资助:

    西南民族大学研究生创新(No.CX2015SZ045)和四川省教育厅(No.15ZB0487)资助项目.

A Concisely Convergent Synthesis of Berberine Chloride

Chen Chenga, Xu Mengmenga, Zhao Qingb, Liu Chengxiuc, Yang Hongjuna, Feng Yuchuana   

  1. a College of Chemistry & Environment Protection Engineering, Southwest University for Nationalities, Chengdu 610041;
    b Preparatory School, Southwest University for Nationalities, Chengdu 610041;
    c Southwest University for Nationalities Hospital, Chengdu 610041
  • Received:2016-12-02 Revised:2017-01-01 Published:2017-01-17
  • Supported by:

    Project supported by the Graduate Innovative Research Projects of Central Universities, Southwest University for Nationalities (No. CX2015SZ045) and the Research Projects Sichuan Provincial Department of Education (No. 15ZB0487).

报道了以1,2-亚甲二氧基苯为起始原料合成盐酸黄连素的汇聚式路线,该路线包括格氏试剂亲核开环、脱保护、环合等5步反应,总收率为33%.该路线反应条件温和、操作简单,且所有中间体及产物都经过1H NMR、13C NMR、MS鉴定.

关键词: 盐酸黄连素, 汇聚式合成, 1,2-亚甲二氧基苯, 格氏试剂

The berberine chloride was synthesized starting from benzo[d][1,3]dioxole with the mild condition and the simple operation in overall 33% yield. The route includes the five steps of nucleophilic ring opening, deprotection and cyclization and so on. All intermediates were determined by 1H NMR, 13C NMR and MS techniques.

Key words: berberine chloride, convergent synthesis, benzo[d][1,3]dioxole, grignard regent