Multicomponent cross-coupling reactions involving alkenes represent a compelling strategy for accessing three-dimensional molecules, a key pursuit in contemporary medicinal chemistry. Transition metal-catalysed processes predominantly necessitate the use of conjugated alkenes or non-activated alkenes equipped with specific auxiliary functional groups, for example, 8-aminoquinoline. However, it remains a huge challenge to directly use unmodified native functional groups, such as alcohols and ethers, as directing groups. Here, by utilizing an anionic bidentate ligand such as acac, we have successfully addressed the challenge of employing weakly coordinating native functional groups as directing groups in a nickel-catalysed cross-coupling of non-activated alkenes. This reaction enables the simultaneous introduction of an sp² fragment and an sp³ fragment to two carbons of the alkenes with high chemo- and regioselectivity. This work demonstrates the advantages and potential of anionic bidentate ligands in the cross-coupling of non-activated alkenes.

涉及烯烃的多组分交叉偶联反应代表了一种令人信服的获取三维分子的策略，这是当代药物化学的一个关键追求。过渡金属催化过程主要需要使用具有特定辅助官能团的共轭烯烃或非活化烯烃，例如8-氨基喹啉。然而，直接使用未修饰的天然官能团（例如醇和醚）作为引导基团仍然是一个巨大的挑战。在这里，通过利用阴离子二齿配体（例如 acac），我们成功解决了在镍催化的非活化烯烃交叉偶联中使用弱配位的天然官能团作为导向基团的挑战。该反应能够以高化学和区域选择性同时将sp ²片段和sp ³片段引入到烯烃的两个碳上。这项工作证明了阴离子二齿配体在非活化烯烃交叉偶联中的优势和潜力。