Iron-catalyzed regioselective alkylation of 1,4-quinones and coumarins with functionalized alkyl bromides.,Organic & Biomolecular Chemistry

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Iron-catalyzed regioselective alkylation of 1,4-quinones and coumarins with functionalized alkyl bromides.
Organic & Biomolecular Chemistry ( IF 2.9 ) Pub Date : 2020-01-08 , DOI: 10.1039/c9ob02289a
Dengke Li ₁ , Xianfu Shen ₂

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A simple and efficient Fe-catalyzed regioselective alkylation of 1,4-quinones and coumarins, using functionalized alkyl bromides as alkylating reagents, has been developed. The reaction proceeds under mild conditions with the addition of alkyl bromides to a wide range of 1,4-quinone and coumarin derivatives with a broad substrate scope and wide functional group tolerance to provide the products in good yields. Further application of these strategies could be extended to important biologically active antimalarial lead drugs, such as plasmodione on a gram scale in a single step for medicinal purposes.

中文翻译：

铁催化的1,4-醌和香豆素的区域选择性烷基化反应。

使用功能化的烷基溴化物作为烷基化试剂，已经开发出一种简单有效的铁催化1,4-醌和香豆素的区域选择性烷基化方法。反应在温和的条件下进行，将烷基溴添加到范围广泛的底物范围和宽泛的官能团耐受性的各种1,4-醌和香豆素衍生物中，可以提供高收率的产物。这些策略的进一步应用可以扩展到重要的具有生物活性的抗疟疾先导药物，例如用于医学目的的克级的plasmodione（克）。

更新日期：2020-02-10

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