Visible Light Assisted Direct C3–H Arylation of Pyrido[1,2-a]pyrimidin-4-ones and Thiazolo[3,2-a]pyrimidin-5-ones,The Journal of Organic Chemistry

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Visible Light Assisted Direct C3–H Arylation of Pyrido[1,2-a]pyrimidin-4-ones and Thiazolo[3,2-a]pyrimidin-5-ones
The Journal of Organic Chemistry ( IF 3.3 ) Pub Date : 2023-05-30 , DOI: 10.1021/acs.joc.3c00780
Rajesh T Bhawale ₁ , Umesh A Kshirsagar ₁

Affiliation

Metal-catalyst-free, organic dye-catalyzed C3–H arylation of pyrido[1,2-a]pyrimidin-4-ones using visible light irradiation was developed under mild reaction conditions. This operationally simple and direct C–H functionalization approach effectively produced biologically significant C3 arylated pyrido[1,2-a]pyrimidin-4-one and thiazolo[3,2-a]pyrimidin-5-one derivatives, including medicinally important endothelial cell dysfunction inhibitor and anti-inflammatory agents in good to excellent yields with good functional group tolerance. The present photoinduced direct C3–H arylation approach was suitable for scale-up synthesis.

中文翻译：

吡啶并[1,2-a]嘧啶-4-酮和噻唑并[3,2-a]嘧啶-5-酮的可见光辅助直接C3-H芳基化

在温和的反应条件下，开发了使用可见光照射的无金属催化剂、有机染料催化的吡啶并[1,2- a ]嘧啶-4-酮的C3-H芳基化。这种操作简单且直接的C-H功能化方法有效地产生了具有生物学意义的C3芳基化吡啶并[1,2- a ]嘧啶-4-一和噻唑并[3,2- a ]嘧啶-5-一衍生物，包括医学上重要的内皮细胞功能障碍抑制剂和抗炎剂的产率良好至优异，且具有良好的官能团耐受性。目前的光诱导直接 C3-H 芳基化方法适合放大合成。

更新日期：2023-05-30

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