有机化学 ›› 2014, Vol. 34 ›› Issue (9): 1759-1765.DOI: 10.6023/cjoc201403041 上一篇    下一篇

综述与进展

维纳卡兰的合成研究进展

叶海伟a, 陈云华a, 周丽萍a, 俞传明b   

  1. a 台州职业技术学院生物与化工学院, 台州 318000;
    b 浙江工业大学药学院, 绿色制药技术与装备教育部重点实验室, 杭州 310014
  • 收稿日期:2014-03-18 修回日期:2014-04-10 出版日期:2014-09-25 发布日期:2014-05-05
  • 通讯作者: 叶海伟 E-mail:yehw@tzvtc.com
  • 基金资助:

    台州市海洋生物资源开发与利用科技创新团队资助(No. MBR2014004)、浙江省研究生创新科研(No. YK2011030)资助项目.

Progresses in Synthesis of Vernakalant

Ye Haiweia, Chen Yunhuaa, Zhou Lipinga, Yu Chuanmingb   

  1. a Department of Biological and Chemical, Taizhou Vocational & Technical College, Taizhou 318000;
    b Key Laboratory of Pharmaceutical Engineering of Ministry of Education, College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou 310014
  • Received:2014-03-18 Revised:2014-04-10 Online:2014-09-25 Published:2014-05-05
  • Supported by:

    Project supported by the Program of Marine Biological Resources Exploitation and Utilization of Science and Technology Innovation Team of Taizhou (No. MBR2014004), and the Innovation Research Foundation of Graduate School of Zhejiang Province (No. YK2011030).

传统的抗心律失常药物疗效较好,但具有致心律失常、器官毒性等副作用. 新上市的维纳卡兰是一种新型抗心律失常药物,为选择性心房钠/钾离子通道阻滞剂,研究表明在新近发作的心房颤动急性转复方面的疗效优于胺碘酮,且临床应用前景较好,对其合成路线进行综述.

关键词: 维纳卡兰, 合成, 研究进展

The traditional antiarrhythmic drug is very efficient, but with arrhythmogenic, organ toxicity and other side effects. Vernakalant is a new antiarrhythmic drug of mixed voltage- and frequency-dependent Na+ and atria-preferred K+ channel blockers. Recent clinical studies show that vernakalant under development for the acute conversion of atrial fibrillation to sinus rhythm is better than amiodarone, so it can be expected to have a good prospect for clinical application. In this review, representative synthetic routes employing chemical or biological resolution and catalytic asymmetric reactions are briefly summarized.

Key words: vernakalant, synthesis, progress