Fast construction of isoquinolin-1(2H)-ones by direct intramolecular C-H/N-H functionalization under metal-free conditions.,Organic & Biomolecular Chemistry

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Fast construction of isoquinolin-1(2H)-ones by direct intramolecular C-H/N-H functionalization under metal-free conditions.
Organic & Biomolecular Chemistry ( IF 2.9 ) Pub Date : 2020-01-02 , DOI: 10.1039/c9ob02430a
Li-Rong Wen ₁ , Guang-Yi Ren , Rui-Sen Geng , Lin-Bao Zhang , Ming Li

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The general protocol for the synthesis of isoxazolidine-fused isoquinolin-1(2H)-ones was established with the help of bench stable hypervalent iodine reagent PIDA. Polycyclic six-, seven- and eight-membered N-heterocycles can be rapidly synthesized from available amides under metal-free conditions within 1 min at room temperature through C-H/N-H functionalization. Moreover, the protocol has the merits of broad substrate scope, atom economy and operational simplicity.

中文翻译：

通过在无金属条件下直接进行分子内CH / NH官能化来快速构建异喹啉-1（2H）-one。

借助台式稳定的高价碘试剂PIDA，建立了合成异恶唑烷融合的异喹啉-1（2H）-的通用方案。多环六元，七元和八元N-杂环可以在室温下1分钟内通过CH / NH官能团在无金属条件下由可用的酰胺快速合成。而且，该协议具有广泛的底物范围，原子经济性和操作简便性的优点。

更新日期：2020-01-02

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