Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 58, Issue 38, Pages 13448-13451Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201907758
Keywords
aza-Heck reaction; catalysis; cyclization; indolines; palladium
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Funding
- University of Delaware (UD)
- NIH NIGMS [NIH P20 GM104316]
- NIH [NIH P20 GM104316, P20 GM104316, P30 GM110758, S10 RR026962, S10 OD016267, NSF CHE-0421224, CHE-0840401, CHE-1229234, CHE-1048367]
- NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES [P30GM110758, P20GM104316] Funding Source: NIH RePORTER
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For the first time, an aza-Heck cyclization that allows the preparation of indoline scaffolds is described. Using N-hydroxy anilines as electrophiles, which can be easily accessed from the corresponding nitroarenes, this method provides indolines bearing pendant functionality and complex ring topologies. Synthesis of challenging indolines, such as those bearing fully substituted carbon atoms at C2, is also possible using this method.
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