Fluorine-containing drugs approved by the FDA in 2019

被引：295

作者：

Mei, Haibo ^{[1
]}

Remete, Attila Mario ^{[2
]}

Zou, Yupiao ^{[1
]}

Moriwaki, Hiroki ^{[3
]}

Fustero, Santos ^{[4
]}

Kiss, Lorand ^{[2
]}

Soloshonok, Vadim A. ^{[5
,6
]}

Han, Jianlin ^{[1
]}

机构：

[1] Nanjing Forestry Univ, Coll Chem Engn, Jiangsu Coinnovat Ctr Efficient Proc & Utilizat F, Nanjing 210037, Peoples R China

[2] Univ Szeged, Inst Pharmaceut Chem, Eotvos U 6, H-6720 Szeged, Hungary

[3] Hamari Chem Ltd, Higashi Yodogawa Ku, 1-4-29 Kunijima, Osaka 5330024, Japan

[4] Univ Valencia, Dept Quim Organ, E-46100 Valencia, Spain

[5] Univ Basque Country, Fac Chem, Dept Organ Chem 1, UPV EHU, Paseo Manuel Lardizabal 3, San Sebastian 20018, Spain

[6] Basque Fdn Sci, Ikerbasque, Maria Diaz de Haro 3,Plaza Bizkaia, Bilbao 48013, Spain

来源：

CHINESE CHEMICAL LETTERS | 2020年 / 31卷 / 09期

基金：

中国国家自然科学基金;

关键词：

Fluorine; Pharmaceuticals; Synthesis; Medicinal chemistry; Marketed medicinal drugs; QUATERNARY STEREOGENIC CENTERS; SELF-DISPROPORTIONATION; ASYMMETRIC-SYNTHESIS; HIGHLY POTENT; AMINO-ACIDS; DISCOVERY; ENANTIOMERS; INHIBITOR; TRIFLUOROMETHYLATION; ENTRECTINIB;

D O I：

10.1016/j.cclet.2020.03.050

中图分类号：

O6 [化学];

学科分类号：

0703 ;

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. ((C) 2020 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.

引用

页码：2401 / 2413

页数：13

共 140 条

[1]

AI-Salama Z.T., 2019, DRUGS, V79, P1477

[2] Siponimod: First Global Approval [J].

Al-Salama, Zaina T. .

DRUGS, 2019, 79 (09) :1009-1015

[3]

Allian A., 2017, [No title captured], Patent No. 2016057372

[4] Alpelisib for PIK3CA-Mutated, Hormone Receptor-Positive Advanced Breast Cancer [J].

Andre, Fabrice ;

Ciruelos, Eva ;

Rubovszky, Gabor ;

Campone, Mario ;

Loibl, Sibylle ;

Rugo, Hope S. ;

Iwata, Hiroji ;

Conte, Pierfranco ;

Mayer, Ingrid A. ;

Kaufman, Bella ;

Yamashita, Toshinari ;

Lu, Yen-Shen ;

Inoue, Kenichi ;

Takahashi, Masato ;

Papai, Zsuzsanna ;

Longin, Anne-Sophie ;

Mills, David ;

Wilke, Celine ;

Hirawat, Samit ;

Juric, Dejan .

NEW ENGLAND JOURNAL OF MEDICINE, 2019, 380 (20) :1929-1940

[5]

Baker W.R., 2000, U.S. Patent

[6]

Bell I.M., 2012, [No title captured], Patent No. 20100122899

[7]

Bell I.M., 2012, [No title captured], Patent No. 2011060081

[8]

Belyk K.M., 2013, [No title captured], Patent No. 2013030696

[9] Deciphering the Fluorine Code-The Many Hats Fluorine Wears in a Protein Environment [J].

Berger, Allison Ann ;

Voeller, Jan-Stefan ;

Budisa, Nediljko ;

Koksch, Beate .

ACCOUNTS OF CHEMICAL RESEARCH, 2017, 50 (09) :2093-2103

[10] Lumateperone: First Approval [J].

Blair, Hannah A. .

DRUGS, 2020, 80 (04) :417-423

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