Oxidative Cross-Dehydrogenative C–H Bond Amination of Imidazo[1,2-a]pyridines in Aqueous Media under Metal-Free Conditions

Synthesis Pub Date : 2024-07-10 DOI:10.1055/a-2348-4764
Durgesh Sarothiya, Umesh A. Kshirsagar
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Abstract

The metal-free direct oxidative cross-dehydrogenative C–H bond amination of imidazopyridines with pyrazole in water as solvent has been developed under K2S2O8-promoted mild conditions. This strategy was applied to variable imidazoheterocycles to give amination products in moderate to good yields. The described protocol also offers scale-up synthesis for the construction of C–N bonds, which makes it suitable for the synthesis of biologically active compounds and pharmaceuticals.

Abstract Image

无金属条件下水介质中咪唑并[1,2-a]吡啶的交叉脱氢 C-H 键氧化胺化反应
在 K2S2O8 促进的温和条件下,开发了咪唑并吡啶与吡唑在水作为溶剂的无金属直接氧化交叉脱氢 C-H 键胺化反应。该方法适用于各种不同的咪唑杂环,能以中等至良好的收率得到胺化产物。所描述的方案还提供了构建 C-N 键的放大合成方法,因此适用于生物活性化合物和药物的合成。
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