| 摘要 |
<p>PROBLEM TO BE SOLVED: To obtain the subject compound in a high yield by reacting a new intermediate obtained from morphinone, codeinone or the like with an alkylating agent, an acylating agent or the like. SOLUTION: A compound of formula I (R<1> is a protecting group; R<2> is a lower alkyl, a lower alkyl substituted by a cycloalkyl or the like; M is an alkali metal, a quaternary ammonium cation) with a compound of the formula: R<3> X (R<3> is a protecting agent; X is a releasing group) to obtain the objective compound of formula II. If necessary, the compound of formula II is reacted with an acid such as tartaric acid to obtain the salt, e.g. ditartarate salt, of the compound of formula II. The compound of the formula: R<3> X is preferably dimethyl sulfate as an alkylating agent, acetyl chloride as an acetylating agent, or the like. The new intermediate of formula I is preferably obtained by reacting a compound of formula III with a compound of the formula: MOR (R is an alkyl) such as potassium t-butoxide. The compound of formula II is preferably thebaine or the like.</p> |
