NEW PRODUCTION OF MOFEZOLAC, MOFEZOLAC NEEDLE-LIKE CRYSTAL AND ITS PRODUCTION

摘要

PROBLEM TO BE SOLVED: To obtain the subject substance known as an antiinflammatory analgesic as a crystal without using an organic solvent as a recrystallization, by maintaining the liquid temperature of an aqueous solution of a mofezolac metal salt such as mofezolac sodium salt in a specific temperature range and adding an acid. ;SOLUTION: 3,4-Di(p-methoxyphenyl)-5-methylisoxazole is reacted with n- butyllithium and carbon dioxide gas to give a mixture, to which water is added. A water layer is collected and treated with a metal chlorinating agent such as sodium chloride to give an aqueous solution of a mofezolac metal salt. The liquid temperature of the aqueous solution is maintained at 65-90°C and an acid in an amount equal to or a little more amount than that of the metal salt is dripped to the aqueous solution to give a cubic crystal of mofezolac having 146°C melting point. The acid concentration is about 1-50%. In the case in which the liquid temperature is 25-65°C to give a needle-like crystal having 126°C melting point. The crystals has the same medicinal effects.;COPYRIGHT: (C)1998,JPO