A PRACTICAL METHOD TO SYNTHESIZE 1,2,3-TRIAZOLE-AMINO-BISPHOSPHONATE DERIVATIVES

作者:Liu, Shuyun; Bi, Wenzhu; Li, Xu; Chen, Xiaolan*; Qu, Lingbo; Zhao, Yufen
来源:Phosphorus, Sulfur, and Silicon and the Related Elements, 2015, 190(11): 1735-1742.
DOI:10.1080/10426507.2015.1012200

摘要

A practical and efficient method for the synthesis of 1,2,3-triazole-amino-bisphosphonates derivatives was developed through two steps: The Michael addition reaction of propargyl amine with vinylidene bisphosphonate, and the 1,3-dipolar click cycloaddition assisted by ultrasound irradiation. This approach has significant advantages in terms of experimental simplicity, mild reaction condition, and can be easily scaled up. The target compounds were characterized by H-1-, P-31-, C-13-NMR spectroscopy and high-resolution mass spectral analyses.