期刊
CHEMISTRY-AN ASIAN JOURNAL
卷 12, 期 18, 页码 2364-2368出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/asia.201700877
关键词
amination; carbene ligands; N-heterocyclic carbenes; N-heteroaryl chlorides; palladium
资金
- National Key R&D Program of China [2016YFA0202902]
- National Natural Science Foundation of China [21572036, 91127041]
- Shanghai International Cooperation Program [14230710600]
- External Cooperation Program of Jiangxi Province [20151BDH80045]
- Department of Chemistry, Fudan University
A series of robust N-heterocyclic carbene palladacycles have been successfully developed. These showed high catalytic activity and selectivity toward the challenging amination of N-heteroaryl chlorides. Different primary and secondary amines were fully compatible with this catalytic system. Remarkably, no double amination products could be detected when primary amines were utilized in our catalytic transformation. Furthermore, the protocol has been successfully extended to synthesize rosiglitazone, a clinical drug for diabetes mellitus, highlighting its potential pharmaceutical feasibility.
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