Fluorine-containing pharmaceuticals approved by the FDA in 2020:Synthesis and biological activity  

作　　者：Yingjie Yu Aiyao Liu Gagan Dhawan Haibo Mei Wei Zhang Kunisuke Izawa Vadim A.Soloshonok Jianlin Han 

机构地区：[1]Jiangsu Co-Innovation Center of Efficient Processing and Utilization of Forest Resources,International Innovation Center for Forest Chemicals and Materials,College of Chemical Engineering,Nanjing Forestry University,Nanjing 210037,China [2]Department of Biomedical Science,Acharya Narendra Dev College,University of Delhi,India [3]Department of Chemistry,University of Massachusetts Boston,100 Morrissey Boulevard,Boston,MA 02125,United States [4]Hamari Chemical Ltd.,1-4-29 Kunijima,Higashi-Yodogawa-ku,Osaka 533-0024,Japan [5]Department of Organic Chemistry I,Faculty of Chemistry,University of the Basque Country UPV/EHU,Paseo Manuel Lardizabal 3,20018 San Sebastian,Spain [6]IKERBASQUE,Basque Foundation for Science,María Díaz de Haro 3,Plaza Bizkaia,48013 Bilbao,Spain

出　　处：《Chinese Chemical Letters》2021年第11期3342-3354,共13页中国化学快报（英文版）

基　　金：the financial support from the National Natural Science Foundation of China(No.21761132021);IKERBASQUE,Basque Foundation for Science.

摘　　要：Thirteen new fluorine-containing drugs,which have been granted approval by the US Food and Drug Administration(FDA)in 2020,are profiled in this review.Therapeutic areas of these new fluorinated pharmaceuticals include medicines and diagnostic agents for Cushing's disease,neurofibromatosis,migraine,Alzheimer's disease,myelodysplastic syndromes,hereditary angioedema attacks,and various cancers.Molecules of these approved drugs feature aromatic fluorine(Ar-F)(11 compounds),aromatic Ar-CF_(3)(1),aliphatic CHF(1)and CF_(2)(1)groups.For each compound,we provide a spectrum of biological activity,medicinal chemistry discovery,and synthetic approaches.

关 键 词：Fluorine and compounds Blockbuster drugs Modern pharmaceuticals SYNTHESIS Drug design and development Asymmetric synthesis 

分 类 号：TQ460.1[化学工程—制药化工]