Kena Zhang, Hui Li, Jingya Li
May 17, 2017
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0
Influential Citations
3
Citations
Journal
Tetrahedron Letters
Abstract
Abstract An efficient protocol for the synthesis of 1-heteroaryl-4-( N -methyl)aminopiperidines starting from heteroaryl chloride derivatives is described. A broad range of 1-heteroaryl-4-( N -Boc- N -methyl)aminopiperidine derivatives were obtained in good to excellent yields using DavePhos as optimal ligand for Pd-catalyzed Buchwald-Hartwig amination reaction. After a mild and efficient acidolysis the amination products could be obtained successfully.