PRODUCTION OF 2-AMINO-4-PYRIDYLMETHYL-6 HYDROXYBENZOTHIAZOLE DERIVATIVE

PURPOSE:To obtain a 2-amino-4-pyridylmethyl-6-hydroxybenzothiazole derivative useful as an agent for preventing and treating diseases for which a lipoxygenase- inhibiting action is effective, by a new method using an amino- pyridylhydroxymethyl-hydroxybenzothazole derivative as a raw material. CONSTITUTION:A 2-amino-4-pyridylhydroxymethyl-6-hydroxybenzothiazole derivative of formula I (R is H, methyl, methoxy; R , R are H, lower alkyl) [e.g. 4-methoxy(3-pyridyl)methyl-6-hydroxy-5,7-dimethyl-2-methylaminobenzoth iazole] is reduced with zinc in acetic acid to obtain the objective compound of formula II. In the reaction, the acetic acid is preferably used in an amount of 1-10 volumes per pt.wt. of the compound of formula I, and the zinc is used in an amount of 2-30 equivalents based on the compound of formula I under refluxing the solvent. The reaction time is usually 6 hrs to 2 days.