Citation: Yingjie Yu, Aiyao Liu, Gagan Dhawan, Haibo Mei, Wei Zhang, Kunisuke Izawa, Vadim A. Soloshonok, Jianlin Han. Fluorine-containing pharmaceuticals approved by the FDA in 2020: Synthesis and biological activity[J]. Chinese Chemical Letters, ;2021, 32(11): 3342-3354. doi: 10.1016/j.cclet.2021.05.042 shu

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

Yingjie Yu ^a ,
Aiyao Liu ^a ,
Gagan Dhawan ^{b, *,} ,
Haibo Mei ^a ,
Wei Zhang ^{c, *,} ,
Kunisuke Izawa ^d ,
Vadim A. Soloshonok ^{e, f, *,} ,
Jianlin Han ^{a, *,}

a.
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
b.
Department of Biomedical Science, Acharya Narendra Dev College, University of Delhi, India
c.
Department of Chemistry, University of Massachusetts Boston, 100 Morrissey Boulevard, Boston, MA 02125, United States
d.
Hamari Chemical Ltd., 1-4-29 Kunijima, Higashi-Yodogawa-ku, Osaka 533-0024, Japan
e.
Department of Organic Chemistry I, Faculty of Chemistry, University of the Basque Country UPV/EHU, Paseo Manuel Lardizábal 3, 20018 San Sebastián, Spain
f.
IKERBASQUE, Basque Foundation for Science, María Díaz de Haro 3, Plaza Bizkaia, 48013 Bilbao, Spain

gagandhawan@andc.du.ac.in

wei2.zhang@umb.edu

vadym.soloshonok@ehu.es

hanjl@njfu.edu.cn

Received Date: 19 March 2021
Revised Date: 21 May 2021
Accepted Date: 21 May 2021
Available Online: 27 May 2021

Figures(22)

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-CF₃ (1), aliphatic CHF (1) and CF₂ (1) groups. For each compound, we provide a spectrum of biological activity, medicinal chemistry discovery, and synthetic approaches.
- Fluorine and compounds,
- Blockbuster drugs,
- Modern pharmaceuticals,
- Synthesis,
- Drug design and development,
- Asymmetric synthesis
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