Solid-Phase Synthesis of 2-Arylamino-5-(4-hydroxyphenyl)-1,3,4-thiadiazole Derivatives Based on Resin-Bound Acylhydrazines

Abstract

A highly efficient, solid-phase synthesis of 2-arylamino-5-(4-hydroxy-phenyl)-1,3,4-thiadiazole derivatives under mild conditions has been developed. The 1,3,4-thiadiazole derivatives were synthesized from resin-bound acylhydrazines in several steps, which gave 78–88% overall yields and excellent purities of the products.

Keywords:

• Resin-bound acylhydrazine
• solid phase synthesis
• 1,3,4-thiadiazole

Acknowledgments

We are grateful to the National Natural Science Foundation of China (Project No. 20802068), the Education Department of Zhejiang Province (20070015), and the Science and Technology Department of Zhejiang Province (2007C2116) for financial support.