通过瞬态配体促进的 3-甲基杂芳醛-2-甲酰基的直接γ-C(sp)-H 芳基化反应来获得杂苄基支架。
Access to Hetero-Benzyl Scaffolds via Transient-Ligand-Enabled Direct γ-C(sp)-H Arylation of 3-Methylheteroarene-2-Carbaldehydes.
机构信息
Department of Chemistry, Indian Institute of Science Education and Research (IISER)-Pune, Dr. Homi Bhabha Road, Pashan, 411008 Pune, Maharashtra, India.
出版信息
J Org Chem. 2020 Jun 5;85(11):6924-6934. doi: 10.1021/acs.joc.0c00154. Epub 2020 May 18.
An efficient and straightforward method has been developed for the synthesis of β-benzyl-substituted 5-membered heterocyclic carbaldehydes via transient directing-group-enabled direct γ-C(sp)-H arylation of 3-methylheteroarene-2-carbaldehydes. A wide range of 3-methylheteroarene carbaldehydes undergo coupling with a variety of aryl iodides, including less reactive iodo pyridine derivatives to provide a library of highly selective functionalized products in good to excellent yields. Some of these products have been successfully utilized in synthesizing useful synthetic intermediates.
本文报道了一种高效、直接的方法，通过 3-甲基杂芳醛-2-甲醛的瞬态导向基团辅助的直接γ-C(sp 3 )-H 芳基化反应，合成了β-苄基取代的五元杂环甲酰化合物。一系列 3-甲基杂芳醛与各种芳基碘化物，包括反应性较低的碘代吡啶衍生物进行偶联，以良好至优异的收率得到了一系列高度选择性的功能化产物库。其中一些产物已成功用于合成有用的合成中间体。
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