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An enantioselective approach to 2,3-disubstituted indolines through consecutive Br?nsted acid/Pd-complex-promoted tandem reactions

机译:通过连续的布朗斯台德酸/钯络合物促进的串联反应对2,3-二取代的二氢吲哚进行对映选择性的方法

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摘要

In tandem: A divergent and enantioselective approach to 2,3-disubstituted indolines was developed through consecutive Br?nsted acid/Pd-complex- promoted tandem reactions from simple 2-substituted indoles and aldehydes in one operation to give up to 98 % ee (see scheme; R~1=H, F, or Me; R ~2=alkyl; R~3=aryl or alkyl). Three Br?nsted acid promoted steps and two Pd-catalyzed hydrogenation steps were involved in this process.
机译:串联:通过一次简单的2-取代的吲哚和醛类的连续布朗斯台德酸/钯-络合物促进的串联反应,开发了一种对2,3-二取代的二氢吲哚的发散和对映选择性的方法,使ee高达98%(参见方案; R〜1 = H,F或Me; R〜2 =烷基; R〜3 =芳基或烷基)。该过程涉及三个布朗斯台德酸促进步骤和两个钯催化的氢化步骤。

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