METHOD FOR PRODUCING COMPOUND USEFUL FOR SYNTHETIC INTERMEDIATE FOR PRODUCING AZOLE ANTIFUNGAL AGENT

摘要

PURPOSE: Provided is a method for producing a compound useful for a synthetic intermediate for producing an azole antifungal agent used in the prevention and treatment of various fungal infection diseases. CONSTITUTION: The compound as a synthetic intermediate for an azole antifungal agent is represented by the following formula(27). The compound of formula(27) is obtained by the method comprising the steps of: reacting a compound represented by formula(12) or a salt thereof with chloromethyl lithium produced from chloroiodomethane or bromochloromethane, or with dimethyl-sulfoxonium methylide, diethyl-sulfoxonium methylide or diethylsulfonium methylide to form a compound of formula(13) or a salt thereof: reacting the compound of formula(13) or a salt thereof with 1,2,4-triazole or imidazole or a salt thereof to form a compound of formula(21) or a salt thereof; and removing the hydroxyl-protecting group Pr from the compound of formula(21) or a salt thereof. In the above formulae, R is methyl; each of R22 and R23 is a fluorine atom; Pr is a hydroxyl-protecting group; and A is CH or N.