Patent ID: 7094904
Filing Date: 2006-08-22
Classification: C07D

Abstract:
1. A process for the synthesis of monohydrate and crystal modifications of fluconazole of formula (I) comprising the steps of: a.) hydrolyzing a silyl ether derivative of formula (II)  wherein the meaning of R then cooling the obtained reaction mixture containing the fluconazole of formula (I) and isolating the precipitated fluconazole monohydrate and optionally dissolving the fluconazole monohydrate obtained from the hydrolysis of silyl-fluconazole in a C b.) dissolving anhydrous fluconazole or monohydrate of it in a C c.) drying slowly fluconazole monohydrate after seeding preferably with seeding crystals of crystal modification II at 30–70° C., preferably in vacuum to obtain the crystal modification II of fluconazole, or d.) drying fast fluconazole monohydrate after seeding preferably with seeding crystals of crystal modification I at 80° C., to obtain the crystal modification I of fluconazole.