NH4I/TBHP-mediated synthesis of 2-aroylbenzothiazoles through [4 + 1] oxidative annulation of 2-aminothiophenols and aryl methyl ketones

Abstract

An efficient one-pot protocol has been established for the synthesis of 2-aroylbenzothiazoles by using the combination of NH₄I/TBHP system. The reaction proceeds through NH₄I/TBHP-mediated oxidation of aryl methyl ketones followed by annulation with sequential CN and CS bond formation. The process demonstrates smooth reactivity across a diverse range of aryl methyl ketones, producing the desired products in good to excellent yields. This method can also be easily scaled up to gram level, resulting in yield of up to 68 %.