含二氟甲基药物及二氟甲基化试剂研究进展  

Research progress on Difluoromethyl-containing drugs and Difluoromethylation reagents

作　　者：陶雪芬[1] 章颖 郑杰锋 王玉新[1] 金银秀[1] 唐富琴[1] TAO Xuefen;ZHANG Ying;ZHENG Jiefeng;WANG Yuxin;JIN Yinxiu;TANG Fuqin(School of Medicine and Pharmaceutical Engineering, Taizhou Vocational & Technical College, Zhejiang Province, Taizhou 310008, China)

机构地区：[1]台州职业技术学院医学与制药工程学院,浙江台州310008

出　　处：《中国医药导报》2019年第11期38-41,共4页China Medical Herald

基　　金：浙江省教科规划项目(2017SCG164);台州职业技术学院一般课题(2017YB06);台州职业技术学院重点课题(2018ZD03)

摘　　要：本文首次介绍了2011～2018年美国FDA批准上市的所有含二氟甲基的药物,并总结了它们的主要临床用途。以化合物的电性效应为基准对国内外文献报道的二氟甲基化试剂进行分类综述,其中较为常见的是亲核二氟甲基化试剂,主要包括TMS类、Ph XCF2H类、Br CF2PO(OEt)2、苯磺酰二氟甲基类和苯磺酰二氟乙酸金属盐类,而亲电二氟甲基化试剂的研究和应用相对较少,已报道的主要有二氟甲基自由基供体和二氟有机金属盐类。This paper presentes all Difluoromethyl-containing drugs approved by FDA in the United States from 2011 to 2018 for the first time. And briefly introduces their clinical applications. The Difluoromethylation reagents reported domestic and foreign are reviewed and classified based on their electrical effect. Among them, the nucleophilic difluoromethylation reagents are the most common ones. They mainly include TMS, PhXCF2H, BrCF2PO(OEt)2, Phenylsulfonyl and Phenylsulfonyl Difluoroacetic acid metal salts. The researches on electrophilic Difluoromethylation reagents are relatively fewer. Difluoromethyl radical donors and Difluorometallic salts have been reported.

关 键 词：含氟药物 亲核二氟甲基化试剂 亲电二氟甲基化试剂 二氟甲基自由基供体 

分 类 号：R914[医药卫生—药物化学]