CuI/l-proline-catalyzed cross-coupling of 2-halotrifluoroacetanilides with beta-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.
Facile Access to Polysubstituted Indoles via a Cascade Cu-Catalyzed Arylation-Condensation Process. Publishing Authors By Initials
Facile Access to Polysubstituted Indoles via a Cascade Cu-Catalyzed Arylation-Condensation Process. Journal Published:
PUBLICATION TYPE: Journal Article
Journal: The Journal of organic chemistry
VOLUME: 72
Page Numbers: 9329-34
Journal Abbreviation: J. Org. Chem.
ISSN: 0022-3263
DAY: 2
MONTH: 11
YEAR: 2007
Facile Access to Polysubstituted Indoles via a Cascade Cu-Catalyzed Arylation-Condensation Process. Information
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LANGUAGE: eng
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AFFILIATION: Department of Chemistry, Fudan University, Shanghai 200433, China, and State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Lu, Shanghai 200032, China.
Country: United States
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MEDLINETA: J Org Chem
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