Publisher： John Wiley & Sons Inc
E-ISSN： 1521-3773|54|51|15400-15404
ISSN： 1433-7851
Source： ANGEWANDTE CHEMIE INTERNATIONAL EDITION, Vol.54, Iss.51, 2015-12, pp. : 15400-15404
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Abstract
AbstractThe 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.
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