大学化学 >> 2018, Vol. 33 >> Issue (7): 43-55.doi: 10.3866/PKU.DXHX201803060

所属专题: 化学科普

科普 上一篇    下一篇

降压药尼莫地平的前世今生

章慧*()   

  • 收稿日期:2018-03-28 发布日期:2018-07-17
  • 通讯作者: 章慧 E-mail:huizhang@xmu.edu.cn
  • 基金资助:
    国家基础科学人才培养基金(J1310024);国家自然科学基金(21273175)

Past and Present of Nimodipine as Hypotensor

Hui ZHANG*()   

  • Received:2018-03-28 Published:2018-07-17
  • Contact: Hui ZHANG E-mail:huizhang@xmu.edu.cn
  • Supported by:
    国家基础科学人才培养基金(J1310024);国家自然科学基金(21273175)

摘要:

以降压药1,4-二氢吡啶衍生物尼莫地平的发现和应用为线索,简要回顾了19世纪中叶以来欧洲立体化学的发展史,主要涉及韩奇酯的发明、韩奇与配位化学创始人维尔纳的师生情谊以及维尔纳对手性立体化学的开拓性贡献等历史故事,介绍了最近的消旋尼莫地平结晶过程中的自发拆分及其手性晶型的精准表征,以及多晶型现象和晶型药物的相关知识。

关键词: 手性立体化学, 韩奇反应, 降压药, 多晶型, 自发拆分

Abstract:

Following the discovery and application of 1, 4-dihydropyridines nimodipine as the antihypertensive drug, this article briefly reviews the development of stereochemistry in Europe since the middle of the 19th century. Chemical stories are introduced, involving the invention of Hantzsch esters, close relationship between Hantzsch and his outstanding student-the founder of Coordination Chemistry-Werner, and Werner's pioneering contribution to chiral stereochemistry. An up-to-date introduction is given for the spontaneous resolution of racemic nimodipine under chiral crystallization and its precise characterization. Moreover, polymorphism and polymorphic drugs have been also described.

Key words: Chiral stereochemistry, Hantzsch reaction, Hypotensor, Polymorphism, Spontaneous resolution

MSC2000: 

  • G64