GB2450691A — One-pot preparation of oxycodone from thebaine

USPTO Abstract

A process for the large scale preparation of oxycodone from thebaine which comprises: <SL> <LI>(i) oxidation of thebaine to 14-hydroxycodeinone with a peroxide; and <LI>(ii) reduction of 14-hydroxycodeinone with hydrogen, characterised in that: <LI>(iii) the oxidation reaction is carried out on more than 50g of thebaine, and <LI>(iv) both the oxidation and reduction reactions are carried out in acetic acid or propionic acid; and <LI>(v) both the oxidation and reduction reactions are carried out in the same vessel without isolation of the 14-hydroxycodeinone; and <LI>(vi) the oxidation reaction is performed at a temperature below 35{C. </SL> Glacial acetic acid and hydrogen peroxide are preferably used in the oxidation reaction. Preferred catalysts for the hydrogenation include palladium on carbon (Pd/C), platinum dioxide and Raney nickel.