Atroposelective Synthesis of Tetrahydropyrrolo[3,2-c]azepine Derivatives Through Gold(I)-Catalyzed Hydroarylation,Advanced Synthesis & Catalysis

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Atroposelective Synthesis of Tetrahydropyrrolo[3,2-c]azepine Derivatives Through Gold(I)-Catalyzed Hydroarylation
Advanced Synthesis & Catalysis ( IF 4.4 ) Pub Date : 2022-11-08 , DOI: 10.1002/adsc.202200828
Quentin Gaignard-Gaillard ₁ , Xu Han ₂ , Aurélien Alix ₁ , Christophe Bour ₃ , Regis Guillot ₄ , vincent gandon ₅ , Arnaud Voituriez ₆

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A series of enantioenriched substituted tetrahydropyrrolo[3,2-c]azepine products possessing an axial chirality were synthesized in 63–99% yield through a gold(I)-catalyzed hydroarylation. DFT calculations rationalized the reactivity observed for the formation of such complex molecular frameworks and guided our choice in the pyrrole N-substituent to isolate configurationally stable compounds.

中文翻译：

金(I)催化加氢芳基化反应选择性合成四氢吡咯并[3,2-c]氮杂衍生物

通过金 (I) 催化的加氢芳基化反应，合成了一系列具有轴向手性的对映体富集取代四氢吡咯并[3,2- c ]氮杂产品，产率为 63-99%。DFT 计算使观察到的形成此类复杂分子框架的反应性合理化，并指导我们选择吡咯N-取代基以分离构型稳定的化合物。

更新日期：2022-11-08

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