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<p>1,3,4-Oxadiazoles are privileged heterocyclic scaffolds with broad bioactivities, holding significant importance in pharmaceutical and agrochemical discovery. Herein, we report a novel, efficient, and simple synthetic route to 2-amino-1,3,4-oxadiazoles via NaOH-mediated desulfurative cyclization of hydrazides and isothiocyanates under mild reaction conditions. This developed methodology features broad substrate tolerance, excellent yields, operational simplicity, and mild conditions, providing a straightforward pathway for versatile syntheses of valuable 1,3,4-oxadiazole derivative. Consequently, the present reaction opens an alternative path for the preparation of 1,3,4-oxadiazoles via regioselective cyclization hydrazides and isothiocyanates.</p>

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A new and efficient synthesis of substituted 2-amino-1,3,4-oxadiazoles from isothiocyanates and hydrazides

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年6月21日

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  • Lei Wu,
  • Haiyign Tian,
  • Yuying Zhang,
  • Wenjing Ma,
  • Qi Zhang,
  • Ruiling Chen,
  • Xiuling Chen

摘要

1,3,4-Oxadiazoles are privileged heterocyclic scaffolds with broad bioactivities, holding significant importance in pharmaceutical and agrochemical discovery. Herein, we report a novel, efficient, and simple synthetic route to 2-amino-1,3,4-oxadiazoles via NaOH-mediated desulfurative cyclization of hydrazides and isothiocyanates under mild reaction conditions. This developed methodology features broad substrate tolerance, excellent yields, operational simplicity, and mild conditions, providing a straightforward pathway for versatile syntheses of valuable 1,3,4-oxadiazole derivative. Consequently, the present reaction opens an alternative path for the preparation of 1,3,4-oxadiazoles via regioselective cyclization hydrazides and isothiocyanates.