[EN] A METHOD OF PREPARATION OF OXYCODONE<br/>[FR] MÉTHODE DE SYNTHÈSE DE L'OXYCODONE
申请人:ZENTIVA AS
公开号:WO2006019364A1
公开(公告)日:2006-02-23
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 to C5 alkyl, an alkylaryl, preferably benzyl, methoxybenzyl, or alkyl, 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.
通过将化学式(II)的苦参碱或其类似物(III)与氢过氧化物或过氧酸在草酸存在下与乙酸或甲酸混合物反应,制备化学式(I)的羟考酮的方法。通过加入碱,从生成的结晶沉淀物14-羟基可待因酮草酸盐中释放出化学式(IV)的14-羟基可待因酮,然后在催化剂存在下用氢气加氢转化为羟考酮(I):羟考酮转化为盐酸盐,作为镇痛剂配方中的活性成分。