Fluorine-containing drugs approved by the FDA in 2019

• Published in: Chinese chemical letters Vol. 31; no. 9; pp. 2401 - 2413
• Main Authors: Mei, Haibo, Remete, Attila Márió, Zou, Yupiao, Moriwaki, Hiroki, Fustero, Santos, Kiss, Lorand, Soloshonok, Vadim A., Han, Jianlin
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 01.09.2020; Jiangsu Co-Innovation Center of Efficient Processing and Utilization of Forest Resources, College of Chemical Engineering, Nanjing Forestry University, Nanjing 210037, China%University of Szeged, Institute of Pharmaceutical Chemistry, 6720 Szeged, E?tv?s u. 6, Hungary%Hamari Chemicals Ltd., 1-4-29 Kunijima, Higashi-Yodogawa-ku, Osaka 533-0024, Japan%Departamento de Química Orgánica, Universidad de Valencia, 46100 Burjassot, Valencia, Spain%Department of Organic Chemistry Ⅰ, Faculty of Chemistry, University of the Basque Country UPV/EHU, Paseo Manuel Lardizábal 3, 20018 San Sebastián, Spain; IKERBASQUE, Basque Foundation for Science, María Díaz de Haro 3, Plaza Bizkaia, 48013 Bilbao, Spain
• Subjects: Fluorine; Marketed medicinal drugs; Medicinal chemistry; Pharmaceuticals; Synthesis; Medicinal chemistry; Marketed medicinal drugs; Synthesis; Fluorine; Pharmaceuticals
• ISSN: 1001-8417; 1878-5964
• DOI: 10.1016/j.cclet.2020.03.050

Eleven new fluorine-containing FDA-approved pharmaceuticals are discussed. Therapeutic areas of these newly developed fluorinated pharmaceuticals include schizophrenia, migraine, multiple sclerosis, insomnia, rheumatoid arthritis, anti-tuberculosis, breast cancer, lymphoma kinase inhibitor and serotonin receptor antagonist. [Display omitted] 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.