氘代抗心血管病药物的合成研究进展  

Research Progress in The Synthesis of Deuterated Anticardiovascular Drugs

作　　者：陈贤勇 周顺 金鑫 葛真真 周鸣强 赵建强 陈永正 袁伟成 CHEN Xianyong;ZHOU Shun;JIN Xin;GE Zhenzhen;ZHOU Mingqiang;ZHAO Jianqiang;CHEN Yongzheng;YUAN Weicheng(Key Laboratory of Biocatalysis and Chiral Drug Synthesis of Guizhou Province,College of Pharmacy,Zunyi Medical University,Zunyi 563000,China;Chengdu Institute of Organic Chemistry,Chinese Academy of Sciences,Chengdu 610041,China;National Engineering Research Center of Chiral Drugs,Chengdu Likai Chiral Tech Co.,Ltd.,Chengdu 610041,China;Zhejiang Jinhua Conba Bio-Pharm Co.,Ltd.,Jinhua 321016,China)

机构地区：[1]遵义医科大学药学院,贵州省生物催化与手性药物合成重点实验室,贵州遵义563000 [2]中国科学院成都有机化学有限公司,四川成都610041 [3]成都丽凯手性技术有限公司,手性药物国家工程研究中心,四川成都610041 [4]浙江金华康恩贝生物制药有限公司,浙江金华321016

出　　处：《合成化学》2023年第8期641-650,共10页Chinese Journal of Synthetic Chemistry

基　　金：国家自然科学基金资助项目(22171029,21901024,21871252,21801024,21801026)。

摘　　要：对药物分子进行氘代化是目前新药研究的一个热点话题,而心血管疾病作为一种病患众多,难以治愈且死亡率高的疾病,严重威胁着人类健康。考虑到氘代药物具有降低药物代谢速率、延长半衰期及降低毒性等优点,开发新型的氘代抗心血管疾病药物具有重要的科研价值和应用价值。本文综述了近几年氘代抗心血管疾病的合成研究进展,主要包括抗高血压药、血脂调节药、抗凝血药和离子通道调节剂。Deuteration of clinic drug molecules is a hot topic in the field of new drug development.As we all know that cardiovascular disease,as a high incidence of disease with difficult to cure and high mortality,is a serious threat to human health.Compared with non-deuterated drugs,deuterated drugs have some advantages,such as reducing drug metabolism rate,prolonging half-life and reducing toxicity.Therefore,the exploring facile and efficient routes for synthesis of new deuterated anticardiovascular drugs holds important scientific research value and application value.In this paper,we review the recent progress in the synthesis of deuterated anticardiovascular agents,including antihypertensive drugs,lipid modulators,anticoagulants and ion channel modulators.

关 键 词：氘代化 抗心血管药物 药物合成 抗高血压药 血脂调节药 抗凝血药 离子通道调节剂 

分 类 号：O621.3[理学—有机化学] R914.5[理学—化学]