| 摘要 |
PROBLEM TO BE SOLVED: To provide a method of producing a naltrexamine derivative which retains high yield and high stereoselectivity without the need to use sodium cyanoborohydride or a borane-pyridine complex as a reducing agent nor the need to use an alcoholic solvent.SOLUTION: In a method of producing a naltrexamine derivative represented by the general formula (III), naltrexone is reacted with a secondary amine derivative in the presence of an acid to produce an iminium intermediate, which is then reacted with a borane-tert-butylamine complex without adding an alcoholic solvent, to reduce the iminium intermediate. [In the formula, Rand Reach independently represent a phenyl group that may have one or more substituents selected from the group consisting of C1-5 alkyl and alkoxy, hydroxy, halogen, amino and nitro.] |
