Fluorine-Containing Drugs Approved by the FDA in 2018

被引：401

作者：

Mei, Haibo ^{[1
]}

Han, Jianlin ^{[1
]}

Fustero, Santos ^{[2
,3
]}

Medio-Simon, Mercedes ^{[2
,3
]}

Sedgwick, Daniel M. ^{[2
,3
]}

Santi, Claudio ^{[4
]}

Ruzziconi, Renzo ^{[5
]}

Soloshonok, Vadim A. ^{[6
,7
]}

机构：

[1] Nanjing Forestry Univ, Coll Chem Engn, Nanjing 210037, Jiangsu, Peoples R China

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

[3] Ctr Invest Principe Felipe, Lab Mol Organ, Valencia 46012, Spain

[4] Univ Perugia, Dept Phrmaceut Sci, Via Liceo 1, I-06123 Perugia, Italy

[5] Univ Perugia, Dept Chem Biol & Biotechnol, Via Elce di Sotto 8, I-06123 Perugia, Italy

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

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

来源：

CHEMISTRY-A EUROPEAN JOURNAL | 2019年 / 25卷 / 51期

基金：

中国国家自然科学基金;

关键词：

biochemistry; cancer; fluorine; HIV; substitution reactions; SPLEEN TYROSINE KINASE; RESISTANT PROSTATE-CANCER; RESEARCH-AND-DEVELOPMENT; AMINO-ACIDS; SELF-DISPROPORTIONATION; ASYMMETRIC-SYNTHESIS; APALUTAMIDE ARN-509; ANTITUMOR-ACTIVITY; ENANTIOMERS SDE; F-19; NMR;

D O I：

10.1002/chem.201901840

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Over the last two decades, fluorine substitution has become one of the essential structural traits in modern pharmaceuticals. Thus, about half of the most successful drugs (blockbuster drugs) contain fluorine atoms. In this review, we profile 17 fluorine-containing drugs approved by the food and drug administration (FDA) in 2018. The newly approved pharmaceuticals feature several types of aromatic F and CF3, as well as aliphatic (CF2) substitution, offering advances in the treatment of various diseases, including cancer, HIV, malarial and smallpox infections.

引用

页码：11797 / 11819

页数：23

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