Zentiva, A.s.

Vladislav Snuparek

Bohumil Proksa

Lubica Ratkovska

A method of preparation of Oxycodone of formula I by reacting thebaine of formula II, or its analogue of formula III, wherein R represents a Cto Calkyl, an alkylaryl, preferably benzyl, methoxybenzyl, or allyl, with hydrogen peroxide or peroxoacids in the presence of oxalic acid in admixture with acetic or formic acid. From the resulting crystalline precipitate of 14-hydroxycodeinone oxalate, by addition of a base, 14-hydroxycodeinone of formula IV is released, which is hydrogenated with hydrogen in the presence of a catalyst to yield Oxycodone (I): Oxycodone is transformed to hydrochloride, which is used as the active ingredient in analgesic formulations.

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Risnovce, Slovakia

Vladislav Snuparek