| 摘要 |
<p>It is described 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 C2-C5 alkyl, an alkylaryl, preferably benzyl, methoxybenzyl, 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 formulation.</p> |
