瞬态导向基团辅助的钯催化吲哚的C4-炔基化反应
Transient Directing Group-Assisted Palladium-Catalyzed C4-Alkynylation of Indoles.
作者信息
Guo Shuqi, Jiang Huanfeng, Yang Shaorong, Wu Wanqing
机构信息
Key Laboratory of Functional Molecular Engineering of Guangdong Province, School of Chemistry and Chemical Engineering, South China University of Technology, Guangzhou 510640, China.
出版信息
J Org Chem. 2025 Jan 24;90(3):1455-1459. doi: 10.1021/acs.joc.4c02478. Epub 2025 Jan 10.
Pd-catalyzed C4-selective alkynylation of indoles was established by employing glycine as a transient directing group. This reaction exhibits high regioselectivity with the tolerance of a wide scope of functional groups to afford diverse alkynylated indoles in moderate to good yields. Moreover, the readily accessible scale-up synthesis and further decorations to achieve multifunctionalized indoles demonstrate the synthetic potential of this protocol.
通过使用甘氨酸作为瞬态导向基团，建立了钯催化的吲哚C4选择性炔基化反应。该反应具有高区域选择性，能耐受多种官能团，以中等至良好的产率得到各种炔基化吲哚。此外，易于进行的放大合成以及进一步修饰以实现多官能化吲哚，证明了该方法的合成潜力。
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