Aqueous, One-Pot, Three-Component Reaction for Efficient Synthesis of 2-[4-(Arylsulfonyl)piperazin-1-yl]-1,3-benzothiazole, ‑1H-benzimidazole, or -1,3-benzoxazole DerivativesK.D. thanks the Council of Scientific and Industrial Research (CSIR), New Delhi, for financial assistance through the 12th Five Year plan projects “Affordable Cancer Therapeutics (ACT)’’ (CSC 0301) and “Small Molecules in Lead Exploration (SMiLE)” (CSC0111)
Received: 14 May 2017
Accepted after revision: 28 June 2017
03 August 2017 (eFirst)
A simple and efficient synthetic protocol has been developed involving a one-pot three-component reaction of a 2-chlorobenzazole, piperazine, and an arenesulfonyl chloride under aqueous conditions at room temperature in the absence of a catalyst, ligand, or base. By using this protocol, a variety of 2-[4-(arylsulfonyl)piperazin-1-yl]-1,3-benzothiazole, -1H-benzimidazole, and -1,3-benzoxazole derivatives were synthesized in excellent yields.