State Key Laboratory of Natural Medicines, Department of Chemistry, China Pharmaceutical University, Nanjing 210009, P. R. China.
J Org Chem. 2021 Sep 3;86(17):12336-12343. doi: 10.1021/acs.joc.1c01230. Epub 2021 Jul 30.
Through β-activation of alkynoic acid esters with N-heterocyclic carbene catalysis, a formal [3+3] annulation of alkynyl acylazoliums with indolin-3-ones has been developed for the rapid construction of structurally interesting benzofuro[3,2-]pyridin-2-ones with potential bioactivities. This protocol provides a highly efficient and simple method for the synthesis of the target molecules under mild reaction conditions with a wide substrate scope and excellent chemoselectivity. The synthetic utility of this protocol was also demonstrated by the versatile late-stage modifications.
通过 N-杂环卡宾催化炔基酸酯的β-活化，发展了炔基酰基氮杂环卡宾与吲哚啉-3-酮的[3+3]环加成反应，用于快速构建具有潜在生物活性的结构有趣的苯并呋喃并[3,2-]吡啶-2-酮。该方法在温和的反应条件下，具有广泛的底物范围和优异的化学选择性，为目标分子的合成提供了一种高效、简单的方法。该方法的合成实用性还通过多种后期修饰得到了证明。
