Journal
ORGANIC LETTERS
Volume 22, Issue 13, Pages 5051-5056Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.0c01632
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Funding
- Shanghai Institute of Materia Medica, Chinese Academy of Sciences
- National Natural Science Foundation of China [21772211]
- Youth Innovation Promotion Association CAS [2014229, 2018293]
- Institutes for Drug Discovery and Development, Chinese Academy of Sciences [CASIMM0120163006]
- Science and Technology Commission of Shanghai Municipality [17JC1405000]
- Program of Shanghai Academic Research Leader [19XD1424600]
- National Science & Technology Major Project Key New Drug Creation and Manufacturing Program, China [2018ZX09711002-006]
- State Key Laboratory of Natural and Biomimetic Drugs
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A copper-catalyzed oxalamide-directed ortho-C-H amination of anilines has been developed by using 1 atm of air as the sole oxidant. The protocol shows excellent functional group tolerance, and some heterocyclic amines including indole, benzothiophene, benzothiazole, quinoline, isoquinoline, and quinoxaline could be compatible in the reaction. The late-stage diversification of medicinal drugs demonstrates the synthetic utility of this protocol.
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