Add time:09/02/2019 Source:sciencedirect.com
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.
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