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TEMPO-Mediated C-H Amination of Benzoxazoles with N-Heterocycles
Jian Wang1, Jiang-Hua Li1, Yidong Guo1
1Sichuan Industrial Institute of Antibiotics, Chengdu University, Chengdu 610052, China.
Abstract:
The direct amination of benzoxazoles at C2 using N-heterocycles as nitrogen sources has been developed for the first time. Several kinds of inexpensive oxidants and also electricity were effective for this transformation in the presence of 2,2,6,6-tetramethylpiperidine-N-oxyl. This metal-free and operationally simple reaction can afford a variety of important C,N'-linked bis-heteocycles in moderate to good yields under very mild reaction conditions. The in situ generated oxoammonium salt was proved to be important for this transformation.
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