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Facile Access to Polysubstituted Indoles via a Cascade Cu-Catalyzed Arylation−Condensation Process
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Abstract

CuI/l-proline-catalyzed cross-coupling of 2-halotrifluoroacetanilides with β-keto esters and amides followed by in situ acidic hydrolysis delivered 2,3-disubstituted indoles. The halides bearing a strong electron-withdrawing group in the 4-position can undergo in situ basic hydrolysis to provide the corresponding indoles. Polysubstituted indoles can be prepared from substituted 2-halotrifluoroacetanilides with high regioselectivity.
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History
- Published In Issue November 23, 2007
- Received September 19, 2007
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