METHOD FOR MANUFACTURING NOVEL MORPHINAN DERIVATIVE

摘要

PURPOSE: Provided is a method for manufacturing a morphinan derivative which is very effective in preventing cramps and protecting nerves by changing groups at C3 and C17 of morphinan. CONSTITUTION: The method for manufacturing a morphinan derivative of the formula (1) comprises the next steps of: i) methylating dextrometrophan hydrobromide to obtain dextrophan of the formula (3); ii) reacting dextrophan with cyclopropylmethyl bromide or aryl bromide in the presence of hydride sodium to manufacture 3-cyclopropylmethoxy-17-methylmorphinan and 3-aryloxy-17-methylmorphinan; and iii) reacting 3-aryloxy-17-methylmorphinan with 1-chloroethyl chloroformate to obtain 3-aryloxymorphinan of the formula (5). In the formula, R is cyclopropylmethyl or aryl group. R' is a methyl group when R is a cyclopropylmethyl group and is hydrogen when R is an aryl group.