Journal
ORGANIC LETTERS
Volume 16, Issue 1, Pages 42-45Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ol402965d
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Funding
- Chinese NSF [81125021, 81373277]
- State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica [SIMM1302KF-08]
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An intermolecular C-H amination of 1-aryl-1H-pyrazol-5(4H)-ones was achieved under mild reaction conditions, using a low catalyst loading and with a broad scope of aminating reagents. This protocol not only provides the first example of rhodium(III)-catalyzed intermolecular aromatic C H amination directed by an intrinsic functionality of the substrate/product but also features aminating an existing drug with either primary or secondary N-benzoate alkylamines as the coupling partners.
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