Organocatalytic Enantioselective aza‐Friedel‐Crafts Reactions of Pyrazolinone Ketimines with Hydroxyindoles and Electron‐Rich Phenols,Advanced Synthesis & Catalysis

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Organocatalytic Enantioselective aza‐Friedel‐Crafts Reactions of Pyrazolinone Ketimines with Hydroxyindoles and Electron‐Rich Phenols
Advanced Synthesis & Catalysis ( IF 4.4 ) Pub Date : 2018-03-24 , DOI: 10.1002/adsc.201800181
Zhong-Tao Yang ₁ , Wu-Lin Yang ₁ , Long Chen ₁ , Hao Sun ₁ , Wei-Ping Deng ₁

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A variety of enantioenriched indole derivatives substituted in the benzene ring were synthesised via an organocatalytic asymmetric aza‐Friedel‐Crafts reaction of pyrazolinone ketimines with hydroxyindoles. This reaction was also applicabled to electron‐rich phenols, yielding the desired products in high yields (up to 99%) and excellent stereo‐selectivities (91–99% ee). Moreover, this method presents its potential in the synthesis of structurally novel indole‐pyrazolinone conjugate derivatives.

中文翻译：

吡唑啉酮酮亚胺与羟基吲哚和富电子苯酚的有机催化对映选择性氮杂-Friedel-Crafts反应

通过吡唑啉酮酮亚胺与羟基吲哚的有机催化不对称氮杂-Friedel-Crafts反应合成了多种被苯环取代的对映体富集的吲哚衍生物。该反应也适用于富电子的苯酚，以高收率（高达99％）和出色的立体选择性（91-99％ee）产生所需的产物。此外，该方法在合成结构新颖的吲哚-吡唑啉酮共轭衍生物方面具有潜力。

更新日期：2018-03-24

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