PREPARATION OF MUSIMOL DERIVATIVE

摘要

PURPOSE:To obtain the title compound useful as a medicine having a psychotropic action in short steps, starting from a readily available 3-hydroxy-5-methylisoxazole. CONSTITUTION:A compound of formula I: (R is H, aryl, or halogen) is reacted with a compound of the formula R'-X (R' is acyl or benzenesulfonyl group; X is halogen) to give a compound of formula II, Which is brominated with N-bromo- succinimide, etc., to form a compound of formula III. The resulting compound is aminated with conc. aqueous anmonia, and the protecting group R' is eliminated to give a musimol of formula IV and its derivative, which is an antiepileptic or cerebral physiological study reagent. The method requires a readily available raw material, produced in large amounts as a pesticide, short steps, and the amination step at normal temperature and pressure. The intermediate is not necessarily purified.