Journal
ORGANIC LETTERS
Volume 23, Issue 21, Pages 8505-8509Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.1c03223
Keywords
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Funding
- Shanghai Institute of Materia Medica
- Chinese Academy of Sciences
- National Natural Science Foundation of China [21772211, 21920102003]
- 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, 21ZR1475400, 18431907100]
- Program of Shanghai Academic Research Leader [19XD1424600]
- National Science & Technology Major Project Key New Drug Creation and Manufacturing Program, China [2018ZX09711002-006]
- China Postdoctoral Science Foundation [2019M662854]
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A copper-mediated ortho-C-H amination of anilines using oxalamide as the directing group and DMF as the amination reagent is reported in this study. The protocol shows good heterocyclic compatibility and synthetic practicality, with mechanistic experiments suggesting a radical pathway may be involved in the reaction.
We report herein a copper-mediated ortho-C-H amination of anilines using oxalamide as the directing group and DMF as the amination reagent. This protocol tolerates various functional groups and shows good heterocyclic compatibility. Late-stage dimethylamination of drugs demonstrated the synthetic practicality of the protocol. Mechanistic experiments indicate that a radical pathway may be involved in the reaction.
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