A [4+1] Cyclative Capture Approach to 3H-Indole-N-oxides at Room Temperature by Rhodium(III)-Catalyzed CH Activation.
A [4+1] Cyclative Capture Approach to 3H-Indole-N-oxides at Room Temperature by Rhodium(III)-Catalyzed CH Activation.
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DOI：
10.1002/anie.201508702
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发表时间：
2015-12
影响因子：
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通讯作者：
Ya-xi Yang;Xuan Wang;Yuanchao Li;Bing Zhou
中科院分区：
文献类型：
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作者：
Ya-xi Yang;Xuan Wang;Yuanchao Li;Bing Zhou
The rhodium(III)-catalyzed [3+2] CH cyclization of aniline derivatives and internal alkynes represents a useful contribution to straightforward synthesis of indoles. However, there is no report on the more challenging synthesis of pharmaceutically important N-hydroxyindoles and 3H-indole-N-oxides. Reported herein is the first rhodium(III)-catalyzed [4+1] CH oxidative cyclization of nitrones with diazo compounds to access 3H-indole-N-oxides. More significantly, this reaction proceeds at room temperature and has been extended to the synthesis of N-hydroxyindoles and N-hydroxyindolines.
