State Key Laboratory of Elemento-Organic Chemistry, Research Institute of Elemento-Organic Chemistry, College of Chemistry, Nankai University, Tianjin 300071, People's Republic of China.
Frontiers Science Center for New Organic Matter, College of Chemistry, Nankai University, Tianjin 300071, People's Republic of China.
Org Lett. 2022 Sep 16;24(36):6599-6603. doi: 10.1021/acs.orglett.2c02595. Epub 2022 Sep 2.
1,2,3-Thiadiazoles are among the most important heterocyclic motifs, with wide applications in natural products and medicinal chemistry. Herein, we disclose a tandem reaction for the synthesis of structurally diverse 1,2,3-thiadiazoles from 3,4-dichloroisothiazol-5-ketones and hydrazines. This method is characterized by mild external oxidant- and sulter-free reaction conditions, a broad substrate scope, and easy purification.
1,2,3-噻二唑是最重要的杂环基序之一,在天然产物和药物化学中有广泛的应用。在此,我们公开了一种从 3,4-二氯异噻唑-5-酮和肼合成结构多样的 1,2,3-噻二唑的串联反应。该方法的特点是温和的外部氧化剂和硫醚反应条件、广泛的底物范围和易于纯化。