期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 56, 期 14, 页码 3966-3971出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201612599
关键词
arylation; copper; indoles; palladium; regioselectivity
资金
- 1000 Youth Talents Plan
- Jiangsu Specially Appointed Professor Plan
- NSF of China [2167020084, 21401099]
An effective and practical strategy has been established for the direct and site-selective arylation of indoles at the C4 and C5 positions with the aid of a readily accessible, cheap, and removable pivaloyl directing group at the C3 position. This transformation shows good functional-group tolerance and could serve as a powerful synthetic tool for the synthesis of medicinally relevant compounds. This method and those developed in previous research together enable the regiocontrolled direct arylation of indole at each C-H bond without prefunctionalization of the reactive sites.
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