Regioselective Alkylation of Thiazolylsulfonamides: Direct and Efficient Synthesis of 3‐Alkylthiazolidene Derivatives

Abstract

Various N‐3‐alkylated thiazolidenesulfonamide derivatives were efficiently prepared by the direct endo‐selective alkylation of thiazolylsulfonamides. The effects of different bases and solvents were investigated, and the NaH–THF combination was found to be the most effective at conferring high yields and endo‐selectivity.

Keywords:

• Alkylation
• alkyl halide
• regioselective
• sulfonamide

Acknowledgment

We acknowledge helpful discussion with Susumu Igarashi. We also thank members of the Division of Analytical Research for performing instrumental analysis.