[5+1] Annulation of aza-o-Quinone Methides with Primary Amines: Construction of 3,4-Dihydroquinazolin-2(1H)-One Derivatives,European Journal of Organic Chemistry

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[5+1] Annulation of aza-o-Quinone Methides with Primary Amines: Construction of 3,4-Dihydroquinazolin-2(1H)-One Derivatives
European Journal of Organic Chemistry ( IF 2.5 ) Pub Date : 2025-03-13 , DOI: 10.1002/ejoc.202500267
Gang Wang ₁ , Hao-Bin Liu ₁ , Zhao-Lin He ₂

Affiliation

A [5+1] annulation reaction between in situ generated aza-o-quinone methides and primary amines has been successfully realized. This approach facilitates the efficient synthesis of a diverse range of 3,4-dihydroquinazolin-2(1H)-one derivatives, exhibiting excellent functional group compatibility. Moreover, the utility of this methodology is further demonstrated by its application in the synthesis of a potential CDK5 inhibitor, a biologically active compound.

中文翻译：

[5+1]氮杂-邻醌二酯与伯胺的环化：3,4-二氢喹唑啉-2（1H）-酮衍生物的构建

原位生成的氮杂-邻醌均化物与伯胺之间的 [5+1] 环化反应已成功实现。该方法有助于高效合成多种 3,4-二氢喹唑啉-2（1H）-酮衍生物，表现出优异的官能团相容性。此外，该方法在合成潜在的 CDK5 抑制剂（一种生物活性化合物）中的应用进一步证明了该方法的实用性。

更新日期：2025-03-13

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