Here, we report a novel strategy for the preparation of diverse heterocycles via a Pd-catalyzed migratory 1,1-cycloannulation reaction (MCAR) of alkenes. Starting from readily available alkenyl amines and alkenyl alcohols, this approach allows the formation of a wide range of five- to seven-membered azaheterocycles and oxaheterocycles with high efficiency and good functional group tolerance. The key to the realization of this reaction is the use of 4-iodophenol or 2-iodophenol derivatives where the phenolic hydroxyl group plays a critical role in controlling the direction of migration and the ring-size of the heterocycles through the formation of a quinone methide intermediate.

中文翻译：

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Pd催化的烯烃迁移1,1-环环化反应


在这里，我们报道了一种通过 Pd 催化的烯烃迁移 1,1-环环化反应 （MCAR） 制备多种杂环的新策略。从现成的烯基胺和烯醇开始，这种方法可以形成广泛的五至七元氮杂杂环和氧杂环，具有高效率和良好的官能团耐受性。实现该反应的关键是使用 4-碘酚或 2-碘酚衍生物，其中酚羟基通过形成醌甲基化物中间体，在控制迁移方向和杂环的环大小方面起关键作用。