PROCESS FOR PREPARING ANTIFUNGAL AZOLE WITH HYDRAZINO AND AMIDRAZONE INTERMIDIATES USING HYDRAZINO AND AMIDRAZOLE INTERMEDIATES

摘要

The present invention relates to a process for the preparation of an antifungal azole compound of formula (I), wherein the epoxide is reacted with hydrazine to form a hydrazino compound, which is then reacted with an imino ether. The amidrazone product is then reacted with orthoportmate to produce an antifungal azole. Known as ZD0870, salicylate exhibits excellent activity against fungal infections in humans, including Candida albaccans, Cryptococcus neo-potentans and Aspergillus fumigatus.