Mao-Tsu Fuh, Ching-Chun Tseng, Sin-Min Li, Shuo-En Tsai, Tsung-Jui Chuang, Chih-Hao Lu, Ya-Chen Yang, Henry J Tsai, Fung Fuh Wong
Through modification of the skeleton of Sitagliptin and Vildagliptin, we successfully synthesized and built-up four series of 1,2,4-triazole derivatives, containing N,O-disubstituted glycolamide, N,N'-disubstituted glycinamide, β-amino ester, and β-amino amide as linkers, for the development of new dipeptidyl peptidase 4 (DPP-4) inhibitors. The synthetic strategy for glycolamides or glycinamides involved convenient two-steps reaction: functionalized transformation of 2-chloro-N-(2,4,5-triflurophenyl)acetamide 9 (hydroxylation or amination) and esterification or amidation of 1,2,4-triazole-3-carboxylic acid...
May 31, 2021: Bioorganic Chemistry