Large-scale oxidations in the pharmaceutical industry

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.