Fluorine in health care Organofluorine containing blockbuster drugs

被引:761
作者
O'Hagan, David [1 ,2 ]
机构
[1] Univ St Andrews, Sch Chem, St Andrews KY16 9ST, Fife, Scotland
[2] Univ St Andrews, Ctr Biomol Sci, St Andrews KY16 9ST, Fife, Scotland
关键词
Organofluorine drugs; Statins; Anti inflammatory; Antacids; Seritonin selective reuptake inhibitors; Neuroleptics; Antibiotics; HMG-COA REDUCTASE; ENANTIOSELECTIVE SYNTHESIS; KEY INTERMEDIATE; INHIBITORS; LANSOPRAZOLE; LEVOFLOXACIN; EFFICIENT; ANALOGS; SERIES;
D O I
10.1016/j.jfluchem.2010.03.003
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
Organic fluorine compounds have had a profound impact on the development of bioactives for the modern pharmaceuticals market It is estimated that up to 20% of pharmaceuticals prescribed or administered in the clinic contain a fluorine atom and 30% of the leading 30 blockbuster drugs by sales contain a fluorine In this Highlight review the top 10 fluorine containing pharmaceuticals (by US Sales in 2008) are highlighted By this measure these are currently the most significant fluorinated compounds impacting on health care They embrace statins (Lipitor Crestor Vytorin Zetia/Ezetimibe) anti-inflammatories (fluticasone propionate Celebrex) antacid (Prevacid) antidepressants (Lexapro) neuroleptics (Risperdal) and antibiotics (Levaquin) In each case the structures and modes of action of these important drugs compounds are reviewed and representative synthetic routes are highlighted (C) 2010 Published by Elsevier BV
引用
收藏
页码:1071 / 1081
页数:11
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