Org Lett. 2021 Jan 1;23(1):183-189. doi: 10.1021/acs.orglett.0c03907. Epub 2020 Dec 18.
Here, we report an unprecedented regioselective, intermolecular 1,2-cyanoalkylacylation of feedstock alkenes with readily available oxime esters and aldehydes by -heterocyclic carbene (NHC) organocatalysis. The crux of this success is the exquisite control over the radical relay process by an NHC organocatalyst. This protocol offers a general platform for diversity-oriented synthesis of valuable ketonitriles under mild, transition-metal-free, and redox-neutral conditions and highlights its potential in the late-stage functionalization of pharmaceutical architectures and natural products.
在这里，我们报告了一种前所未有的通过 -杂环卡宾（NHC）有机催化，对易得的肟酯和醛与原料烯烃进行区域选择性、分子间 1,2-氰基烷基酰化反应。这一成功的关键是通过 NHC 有机催化剂对自由基接力过程的精确控制。该方案为在温和、无过渡金属和氧化还原中性条件下进行有价值的酮腈的多样性导向合成提供了一个通用平台，并突出了其在药物结构和天然产物的后期官能化中的潜力。
