Large-scale oxidations in the pharmaceutical industry

被引:732
作者
Caron, Stephane [1 ]
Dugger, Robert W. [1 ]
Ruggeri, Sally Gut [1 ]
Ragan, John A. [1 ]
Ripin, David H. Brown [1 ]
机构
[1] Pfizer Inc, Chem Res & Dev, Pfizer Global Res Div, Groton, CT 06340 USA
关键词
D O I
10.1021/cr040679f
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Oxidation reactions are powerful tools to convert a position that is protected in a lower oxidation state to the desired functionality and for the functionalization of otherwise unfunctionalized positions. Despite their power as a synthetic tool, these reactions are not fully utilized in the pharmaceutical industry. To illustrate the reasons for this hesitation, an overview is given of the currently acceptable methods for large-scale oxidations of alkenes, arenes, alkylarenes, alcohols, amines, sulfides, and other substrates. It is shown that the Moffat oxidation and TEMPO-based oxidants are especially valuable for the conversion of primary alcohols into aldehydes.
引用
收藏
页码:2943 / 2989
页数:47
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