Alkylated heteroarenes are widely found in bioactive molecules and pharmaceuticals. Therefore, there is great interest in developing a chemoselective alkylation of heteroarenes under mild conditions, particularly during a late-stage functionalization step for the purpose of rapid derivatization. Herein, we introduce an efficient visible-light-promoted C–H alkylation of nitrogen-containing heteroarenes by using C4-alkyl 1,4-dihydropyridines (DHPs) as radical precursors at ambient temperatures. A broad scope of heteroarenes, such as 4-hydroxyquinazoline and its derivatives, including those bearing electron-donating or electron-withdrawing groups, can be successfully alkylated in good yields by using various C4-alkyl DHPs.

烷基化的杂芳烃广泛存在于生物活性分子和药物中。因此，在温和的条件下，特别是在为了快速衍生化的后期官能化步骤期间，开发杂芳烃的化学选择性烷基化引起了极大的兴趣。本文中，我们通过在环境温度下使用C4-烷基1,4-二氢吡啶（DHP）作为自由基前体，引入了一种有效的可见光促进含氮杂芳烃的CH烷基化反应。通过使用各种C4-烷基DHP，可以成功地烷基化各种杂芳烃，例如4-羟基喹唑啉及其衍生物，包括带有给电子或吸电子基团的杂芳烃。