Ma Yu-zhuo
2011
Citations
0
Influential Citations
0
Citations
Journal
Journal of Guangdong Pharmaceutical University
Abstract
Objective To synthesize the key intermediate 4-amino-4-methylpiperidine di-p-toluenesulfonate of ABT-279 and K-579,which are potential dipeptidyl peptidase-4 inhibitors.Methods The key intermediate was prepared starting from ethyl piperidine-4-carboxylate via N-Boc protection,alkylation,amidation,Hofmann rearrangement and N-Boc deprotection.Results The overall yield of process was 49.5%.Conclusion This synthetic process is suitable for large scale preparation with a higher yield,lower cost and simplified operation.