Hydroxyisothiazoles. II. Preparation of isothiazolin-3-ones and their methylated derivatives from the oxidation of cyano-substituted dithioacetate salts

Abstract

The hydrogen peroxide oxidation of α-cyanoaryldithioacetate salts (3) affords substituted isothiazol-3-ols (isothiazolin-3-ones) (4) in moderate yields. Methylation of the products yields mainly N-methyl derivatives. 4-Arylisothiazol-3-ols can be further oxidized to saccharin analogues (7).