Facile Access to Polysubstituted Indoles via a Cascade Cu-Catalyzed Arylation-Condensation Process
Yu Chen, Xiaoan Xie and Dawei Ma*
*State Key Laboratory of Bioorganic and Natural Products
Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences,
354 Fenglin Lu, Shanghai 200032, China, Email: madw
mail.sioc.ac.cn
Y. Chen, X. Xie, D. Ma, J. Org. Chem., 2007, 72, 9329-9334.
DOI: 10.1021/jo702059q
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Abstract
CuI/l-proline-catalyzed cross-coupling of 2-halotrifluoroacetanilides with β-keto esters and amides followed by acidic hydrolysis delivered 2,3-disubstituted indoles. 2-halotrifluoroacetanilides bearing a strong electron-withdrawing group in the 4-position can undergo in situ basic hydrolysis to provide the corresponding indoles.
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F. Liu, D. Ma, J. Org. Chem., 2007, 72, 4844-4850.
Key Words
ID: J42-Y2007-3680
