p-TsOH-Mediated Intramolecular C2-Arylation on NH-Indoles: Access of 5,10-Dihydroindeno[1,2-b]indoles,Organic Letters

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p-TsOH-Mediated Intramolecular C2-Arylation on NH-Indoles: Access of 5,10-Dihydroindeno[1,2-b]indoles
Organic Letters ( IF 4.9 ) Pub Date : 2024-08-05 , DOI: 10.1021/acs.orglett.4c02051
Anurag Verma _{1,

2} , Ruchir Kant ₃ , Nayan Ghosh _{1,

2}

Affiliation

5,10-Dihydroindeno[1,2-b]indole has served as an important starting precursor for BARAC-fluor reagent in medicinal chemistry. Herein, an unprecedented p-TsOH assisted intramolecular C2-arylation of NH-indoles via C(sp²)-CN/C(sp²)-H coupling, offering a series of 5,10-dihydroindeno[1,2-b]indoles with moderate to good yields, has been showcased under redox-neutral conditions. Furthermore, successful scalability and synthetic applications highlight the practical nature of the method.

中文翻译：

p-TsOH 介导的 NH-吲哚分子内 C2-芳基化：获得 5,10-二氢茚并[1,2-b]吲哚

5,10-二氢茚并[1,2- b ]吲哚已成为药物化学中BARAC-氟试剂的重要起始前体。在此，前所未有的p -TsOH通过C(sp ² )-CN/C(sp ² )-H偶联辅助NH-吲哚的分子内C2-芳基化，提供了一系列5,10-二氢茚并[1,2- b ]在氧化还原中性条件下，吲哚具有中等至良好的产率。此外，成功的可扩展性和合成应用凸显了该方法的实用性。

更新日期：2024-08-05

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