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Fluorine-containing drugs approved by the FDA in 2021

Chinese Chemical Letters 2023年第1期34卷 29-38页

作者： Jingrui He Ziyi Li Gagan Dhawan Wei Zhang Alexander E.Sorochinsky Greg Butler Vadim A.Soloshonok Jianlin Han Jiangsu Co-Innovation Center of Efficient Processing and Utilization of Forest Resources International Innovation Center for Forest Chemicals and MaterialsCollege of Chemical EngineeringNanjing Forestry UniversityNanjing 210037China Department of Biomedical Science Acharya Narendra Dev CollegeUniversity of DelhiNew Delhi 110019India Department of Chemistry University of Massachusetts BostonBostonMA 02125United States V.P.Kukhar Institute of Bioorganic Chemistry and Petrochemistry The National Academy of Sciences of UkraineKyiv 02094Ukraine Oakwood Chemical Inc.EstillSC 29918United States Department of Organic Chemistry I Faculty of ChemistryUniversity of the Basque Country UPV/EHU20018 San SebastiánSpain IKERBASQUE Basque Foundation for SciencePlaza Bizkaia48013 BilbaoSpain

Nine new fluorine-containing drugs have been approved by the US Food and Drug Administration(FDA)in 2021,which are presented in this review *** small molecular drugs feature aromatic fluorine,trifluoromethyl and chlorodifluoro *** therapeutic areas of these fluorine-containing drugs include multiple myeloma,lymphoma,HIV,chronic heart failure,chronic myeloid leukemia,(ANCA)-associated vasculitis,migraines,von Hippel-Lindau disease,and non-small cell lung *** brief biological activities and the synthetic methods have been discussed in this review for each of these nine drugs.

关键词： Fluorine-containing compounds blockbuster drugs Pharmaceuticals Anti-cancer Drug design and development Asymmetric synthesis

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FDA approved fluorine-containing drugs in 2023

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Chinese Chemical Letters 2024年第11期35卷 111-122页

作者： Qian Wang Yeping Bian Gagan Dhawan Wei Zhang Alexander E.Sorochinsky Ata Makarem Vadim A.Soloshonok Jianlin Han Jiangsu Co-Innovation Center of Efficient Processing and Utilization of Forest Resources College of Chemical EngineeringNanjing Forestry UniversityNanjing 210037China Jiangsu Province Geriatric Hospital Nanjing 210024China School of Allied Medical Sciences Delhi Skill and Entrepreneurship Universityand Department of Biomedical ScienceAcharya Narendra Dev CollegeUniversity of DelhiNew Delhi 110019India Department of Chemistry University of Massachusetts BostonBostonMA 02125United States V.P.Kukhar Institute of Bioorganic Chemistry and Petrochemistry The National Academy of Sciences of UkraineKyiv 02094Ukraine Department of Chemistry University of HamburgMartin-Luther-King-Platz 6Hamburg 20146Germany Department of Organic Chemistry I Faculty of ChemistryUniversity of the Basque Country UPV/EHUPaseo Manuel Lardizábal 3San Sebastián 20018Spain IKERBASQUE Basque Foundation for ScienceMaría Díaz de Haro 3Plaza BizkaiaBilbao 48013Spain

This review profiles twelve fluorine-containing drugs approved by the US Food and Drug Administration(FDA) for the clinic in *** small molecule drugs represent such therapeutic areas as cancer,neuromuscular disorder,immunodeficiency,virology,and infectious *** chemistry discovery,biological activity,and synthetic routes have been discussed for each ***,new trends in structural positioning,functionality,and degree of fluorination are *** fluorination,the importance of amino acid residues and chirality in the design of new pharmaceuticals is highlighted.

关键词： Fluorine-containing compounds blockbuster drugs Pharmaceuticals Anti-cancer Drug design and development Asymmetric synthesis

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

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Chinese Chemical Letters 2021年第11期32卷 3342-3354页

作者： Yingjie Yu Aiyao Liu Gagan Dhawan Haibo Mei Wei Zhang Kunisuke Izawa Vadim A.Soloshonok Jianlin Han Jiangsu Co-Innovation Center of Efficient Processing and Utilization of Forest Resources International Innovation Center for Forest Chemicals and MaterialsCollege of Chemical EngineeringNanjing Forestry UniversityNanjing 210037China Department of Biomedical Science Acharya Narendra Dev CollegeUniversity of DelhiIndia Department of Chemistry University of Massachusetts Boston100 Morrissey BoulevardBostonMA 02125United States Hamari Chemical Ltd. 1-4-29 KunijimaHigashi-Yodogawa-kuOsaka 533-0024Japan Department of Organic Chemistry I Faculty of ChemistryUniversity of the Basque Country UPV/EHUPaseo Manuel Lardizabal 320018 San SebastianSpain IKERBASQUE Basque Foundation for ScienceMaría Díaz de Haro 3Plaza Bizkaia48013 BilbaoSpain

Thirteen new fluorine-containing drugs,which have been granted approval by the US Food and Drug Administration(FDA)in 2020,are profiled in this *** 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 *** of these approved drugs feature aromatic fluorine(Ar-F)(11 compounds),aromatic Ar-CF_(3)(1),aliphatic CHF(1)and CF_(2)(1)*** 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

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