Synthesis of 5-Amino-1,2,4-triazoles from Carbodiimides with Nitrilimines via 1,3-Dipolar Cycloaddition and Bioactivity Study

• Main Authors: Fang-Chun Kung, 龔芳醇
• Other Authors: Fung-Fuh Wong
• Format: Others
• Language: en_US
• Published: 2014
• Online Access: http://ndltd.ncl.edu.tw/handle/yu5n4s

碩士 === 中國醫藥大學 === 藥物化學研究所碩士班 === 102 === An effective 1,3-dipolar cycloaddition was successfully developed for synthesis 5-amino-1,2,4-triazoles by reacting hydrazonoyl hydrochlorides (nitrilimines) with carbodiimides in the presence of triethylamine as a base catalyst. Carbodiimides can be adapted to the newly developed reaction condition, except for diphenyl carbodiimide. All of 5-Amino-1,2,4-triazoles were evaluated against a panel of human cancer cell lines in vitro, including lung carcinoma (NCI-H226), nasopharyngeal (NPC-TW01), and T-cell leukemia (Jurkat) cells. Based on the IC50, result, most of them provided the poor inhibitory potency.