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铑(III)催化的连续C(sp)-H活化和C(sp)-H胺化引发的分子内级联环化反应。

Intramolecular cascade annulation triggered by rhodium(III)-catalyzed sequential C(sp)-H activation and C(sp)-H amination.

作者信息

Song Liangliang, Tian Guilong, Van der Eycken Johan, Van der Eycken Erik V

机构信息

Laboratory for Organic & Microwave-Assisted Chemistry (LOMAC), Department of Chemistry, KU Leuven, Celestijnenlaan 200F, 3001, Leuven, Belgium.

Laboratory for Organic and Bio-Organic Synthesis, Department of Organic and Macromolecular Chemistry, Ghent University, Krijgslaan 281 (S.4), B-9000 Ghent, Belgium.

出版信息

Beilstein J Org Chem. 2019 Feb 27;15:571-576. doi: 10.3762/bjoc.15.52. eCollection 2019.

Abstract

A rhodium(III)-catalyzed intramolecular oxidative annulation of -substituted -hydroxyacrylamides for the construction of indolizinones via sequential C(sp)-H activation and C(sp)-H amination has been developed. This approach shows excellent functional-group tolerance. The synthesized scaffold forms the core of many natural products with pharmacological relevance.

摘要

已开发出一种铑(III)催化的α-取代的β-羟基丙烯酰胺的分子内氧化环化反应,用于通过连续的C(sp)-H活化和C(sp)-H胺化构建中氮茚酮。该方法显示出优异的官能团耐受性。合成的骨架构成了许多具有药理学相关性的天然产物的核心。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b71/6404421/2318e49ed30a/Beilstein_J_Org_Chem-15-571-g002.jpg

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