Catalyst-free efficient synthesis of functionalized 1,2,4-triazole via ring opening/cyclization of arylidene thiazolone with aryl/alkyl-hydrazine

Abstract

We report a catalyst-free synthesis of hydrazone-substituted 1,2,4-triazoles via ring opening/intramolecular cyclization of arylidene thiazolone by aryl/alkyl-hydrazine. The reaction exhibits a broad substrate scope and is demonstrated on a gram scale in both batch and continuous flow synthesis. Furthermore, the direct one-pot synthesis of indole-substituted 1,2,4-triazole expands its structural diversity.