Fluorine-containing drugs approved by the FDA in 2019  

作　　者：Haibo Mei Attila Mario Remete Yupiao Zou Hiroki Moriwaki Santos Fustero Lorand Kiss Vadim ASoloshonok Jianlin Han 

机构地区：[1]Jiangsu Co-Innovation Center of Efficient Processing and Utilization of Forest Resources,College of Chemical Engineering,Nanjing Forestry University,Nanjing 210037,China [2]University of Szeged,Institute of Pharmaceutical Chemistry,6720 Szeged,Eotvos u.6,Hungary [3]Hamari Chemicals Ltd.,1-4-29 Kunijima,Higashi-Yodogawa-ku,Osaka 533-0024,Japan [4]Departamento de Quimica Organica,Universidad de Valencia,46100 Burjassot,Valencia,Spain [5]Department of Organic Chemistry 1,Faculty of Chemistry,University of the Basque Country UPV/EHU,Paseo Manuel Lardizabal 3,20018 San Sebastian,Spain [6]IKERBASQUE,Basque Foundation for Science.Maria Diaz de Haro 3,Plaza Bizkaia,48013 Bilbao,Spain

出　　处：《Chinese Chemical Letters》2020年第9期2401-2413,共13页中国化学快报（英文版）

基　　金：financial support from the financial support from the National Natural Science Foundation of China(No.21761132021);IKERBASQUE,Basque Foundation for Science;The Hungarian Research Foundation(NKFIH No.K119282);Ministry of Human Capacities,Hungary grant 20391-3/2018/FEKUSTRAT。

摘　　要：Eleven new fluorine-containing FDA-approved drugs have been profiled and details of their discovery and preparation are discussed.Therapeutic areas include schizophrenia,migraine,multiple sclerosis,insomnia,rheumatoid arthritis,anti-tuberculosis,breast cancer,lymphoma kinase inhibitor,serotonin receptor antagonist.New pharmaceuticals feature four examples of aromatic fluorine,three aromatic CF3 group,three aliphatic CF3 and one compound with aromatic CF3O group.Furthermore,among the new compounds,six are chiral and seven are derived from tailor-made amino acids.

关 键 词：FLUORINE Pharmaceuticals SYNTHESIS Medicinal chemistry Marketed medicinal drugs 

分 类 号：TQ460.1[化学工程—制药化工]