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Updated: Jun 17, 2025

Preparation of N-2-alkoxyvinylsulfonamides from N-tosyl-1,2,3-triazoles and Subsequent Conversion to Substituted Phthalans and Phenethylamines
Published on: January 3, 2018
Nickel-catalysed reductive C-N bond cross-coupling between aryl halides and N-chloroamides
Yiting Luo1, Jiacan Yao1, Yunzhi He1
1School of Pharmaceutical Sciences and Yunnan Key Laboratory of Pharmacology for Natural Products; College of Modern Biomedical Industry, Kunming Medical University, 1168 Western Chunrong Road, Yuhua Street, Chenggong District, Kunming City, Yunnan 650500, P. R. China. xuchang@kmmu.edu.cn.
Abstract:
A method for the direct synthesis of N-aryl lactams and amides with aryl halides and N-chloroamides through a Ni-catalyzed reductive C-N coupling reaction has been developed. The reaction features the advantages of mild conditions, good functional group tolerance and broad substrate scope including drug-derived substrates, and also provided direct access to the key synthetic intermediates for some bioactive molecules, suggesting the practicability of this method. Finally, DFT calculations were performed to shed further light on the reaction mechanism and it was found that an amidyl radical might be involved.
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