Palladium-catalyzed coupling reactions on functionalized 2-trifluoromethyl-4-chromenone scaffolds. Synthesis of highly functionalized trifluoromethyl-heterocycles.,Synthesis

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Palladium-catalyzed coupling reactions on functionalized 2-trifluoromethyl-4-chromenone scaffolds. Synthesis of highly functionalized trifluoromethyl-heterocycles.
Synthesis ( IF 2.2 ) Pub Date : 2019-03-01 , DOI: 10.1055/s-0037-1610669
Javier Izquierdo ₁ , Atul D Jain ₁ , Sarki A Abdulkadir _{2,

3} , Gary E Schiltz _{1,

3,

4}

Affiliation

The chromenone core is a ubiquitous group in biologically-active natural products and has been extensively used in organic synthesis. Fluorine derived compounds, including those with a trifluoromethyl group (-CF3), have shown enhanced biological activities in numerous pharmaceuticals compared with their non-fluorinated analogs. We have found that 2-trifluoromethyl chromenones can be readily functionalized in the 8- and 7-positions, providing chromenones cores of high structural complexity which are excellent precursors for numerous trifluoromethyl-heterocycles.

中文翻译：

功能化 2-三氟甲基-4-色烯酮支架上的钯催化偶联反应。高功能化三氟甲基杂环的合成。

色酮核心是具有生物活性的天然产物中普遍存在的基团，已广泛用于有机合成。与非氟化类似物相比，氟衍生化合物，包括具有三氟甲基 (-CF3) 的化合物，在许多药物中显示出增强的生物活性。我们发现2-三氟甲基色酮可以很容易地在8-和7-位上官能化，提供结构复杂性高的色酮核心，这是许多三氟甲基杂环的优异前体。

更新日期：2018-11-20

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