Abstract

Quinazolin-4(3H)-one structures are highly valued in synthetic chemistry due to their incorporation into diverse natural products and drug molecules. Here, we present a new approach for constructing quinazolin-4(3H)-ones utilizing the reactive N-sulfonoketenimines, generated in situ from terminal alkynes and sulfonyl azides and 2-aminobenzamides in the presence of CuI and Et₃N. The reaction proceeded smoothly in MeCN at room temperature to afford the target compounds in good efficiency and amenable to gram-scale synthesis.

Graphical abstract

中文翻译：

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由 N-磺基烯酮亚胺和 2-氨基苯甲酰胺形成喹唑啉-4(3H)-酮

摘要

Quinazolin-4(3 H )-one 结构由于能够融入多种天然产物和药物分子中，因此在合成化学中具有很高的价值。在这里，我们提出了一种利用反应性N -磺基烯酮亚胺构建 quinazolin-4(3 H )-one 的新方法，该反应是在 CuI 和 Et ₃ N存在下由末端炔烃、磺酰叠氮化物和 2-氨基苯甲酰胺原位生成的。室温下在 MeCN 中顺利进行，以良好的效率提供目标化合物，并且适合克级合成。

图形概要