Enantioselective synthesis of indole derivatives by Rh/Pd relay catalysis and their anti-inflammatory evaluation.,Chemical Communications

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Enantioselective synthesis of indole derivatives by Rh/Pd relay catalysis and their anti-inflammatory evaluation.
Chemical Communications ( IF 4.3 ) Pub Date : 2020-05-25 , DOI: 10.1039/d0cc03158e
Sifeng Li ₁ , Zihao Wang ₁ , Haitao Xiao ₂ , Zhaoxiang Bian ₃ , Jun Joelle Wang ₄

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An efficient Rh/Pd relay catalyzed intermolecular and cascade intramolecular hydroamination for the synthesis of exclusive trans 1-indolyl dihydronaphthalenols (up to 88% yield, 99% ee) is described under mild conditions. Moreover, the in silico and in vitro screening showed that the novel 1-indolyl dihydronaphthalenol products are potent lead compounds for treating inflammation disease.

中文翻译：

Rh / Pd中继催化对映体合成吲哚衍生物及其抗炎性评估。

在温和的条件下，描述了一种有效的Rh / Pd接枝催化的分子间和级联分子内胺化反应，可合成独家的反式1-吲哚基二氢萘酚（产率高达88％，ee为99％）。此外，计算机和体外筛选表明，新型的1-吲哚基二氢萘酚产品是用于治疗炎症疾病的有效先导化合物。

更新日期：2020-07-09

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