| 摘要 |
PURPOSE:To obtain a new azole derivative useful as a therapeutic agent for deep mycosis and systemic mycosis, having high safety to human body, showing antifungal action in the case of intravenous injection or oral administration in a liberated state or in the form of salt, having an imidazole ring. CONSTITUTION:1-Aminoimidazole is reacted with an aldehyde shown by formula I [Ar is (substituted) aryl or heterocyclic ring; (n) is 1 or 2] in the presence of an acid catalyst to give a ketoimine derivative of formula II. Then the derivative is reacted with a reducing agent of hydride donating type such as sodium boron hydride and the reaction product is reacted with a haloformic ester of formula X<2>COOR<5> (X<2> is halogen; R<5> is 1-6C alkyl, phenyl, etc.) in the presence of a base to give an imidazole derivative of formula III. Further this derivative is subjected to ring closure reaction in the presence of a strong base such as sodium hydride under heating to give the objective new azole derivative of formula IV (NXY is group of formula V, etc.). |
