Synlett 2017; 28(17): 2295-2298
DOI: 10.1055/s-0036-1590972
© Georg Thieme Verlag Stuttgart · New York

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 Derivatives

Kommula Dileep*, M. S. R. Murty
  • MCP Division, Discovery Building D-203, Indian Institute of Chemical Technology, Uppal Road, Tarnaka, Hyderabad 500607, India   Email:
K.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)
Further Information

Publication History

Received: 14 May 2017

Accepted after revision: 28 June 2017

Publication Date:
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.

Supporting Information