ISOTHIAZOLE DERIVATIVES, PROCESSES FOR PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

摘要

PURPOSE: Isothiazole derivatives, processes for preparing the same, and pharmaceutical compositions containing the same are provided. The isothiazole derivatives have improved fever-removing, pain-alleviating and anti-inflammatory activities and improves adverse side-effects of conventional non-steroidal anti-inflammatory agents. CONSTITUTION: Isothiazole derivatives represented by the formula(1) or non-toxic salts thereof are provided, wherein R1 is hydrogen, alkoxy or halogen; and R2 is methyl or amino. A method for preparing isothiazole derivatives of the formula(1a) comprises reacting a compound of the formula(7) with ammonia water. A method for preparing isothiazole derivatives of the formula(1b) comprises reacting a compound of the formula(7) with hydrazine and iodomethyl. A method for preparing isothiazole derivatives of the formula(1c) comprises reacting a compound of the formula(12) with P2S5 and 2,3,5,6-tetrachloro-1,4-benzoquinone.