Radical Multicomponent Alkyl Alkynylation of Propellane via Synergistic Photoredox and Copper Catalysis,Organic Letters

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Radical Multicomponent Alkyl Alkynylation of Propellane via Synergistic Photoredox and Copper Catalysis
Organic Letters ( IF 4.9 ) Pub Date : 2022-06-21 , DOI: 10.1021/acs.orglett.2c01721
Jie Shi ₁ , Qiao-Lin Xu ₁ , Yu-Qing Ni ₁ , Lin Li ₁ , Fei Pan ₁

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Bicyclo[1.1.1]pentanes (BCPs) are important bioisosteres of aryl, tert-butyl groups, and internal alkynes that can impact key physicochemical properties on drug candidates. Herein, we describe a novel and efficient reaction to synthesize alkyl-alkynyl-substituted BCP derivatives by synergistic photoredox and copper catalysis at room temperature. The mild reaction conditions, simple protocol, broad functional group tolerance, and high efficiency of this procedure make it a valuable strategy for accessing alkynyl-substituted BCPs.

中文翻译：

通过协同光氧化还原和铜催化丙烷自由基多组分烷基炔基化

双环[1.1.1]戊烷 (BCP) 是芳基、叔丁基和内部炔烃的重要生物等排体，可影响候选药物的关键物理化学性质。在此，我们描述了一种在室温下通过协同光氧化还原和铜催化合成烷基-炔基取代的 BCP 衍生物的新型高效反应。该过程温和的反应条件、简单的方案、广泛的官能团耐受性和高效率使其成为获得炔基取代的 BCP 的有价值的策略。

更新日期：2022-06-21

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