1,2,4-triazolo [1,5-a] Pyrimidine Compounds

In this thesis designed and synthesised of a new series of [1,2,4]triazolo[1,5-a]pyrimidine derivatives as epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TKI).The development of receptor-tyro sine kinase inhibitors and EGFR TKIs were reviewed. Based on the analysis of structure-activity relationship of 4-phenylamino quinazoline derivatives and former reasearch work in our Lab, a new series of [1,2,4]triazolo[1,5-a]pyrimidines were designed, and the modifications and optimizations were made on 5-position and 7-position.Starting from ethyl 4-chloro-3-oxobutanoate and 1,2,4-triazol-3-amine, a new synthetic route was developed through cyclization, chlorination, substitution and Mannich reaction. Total 23 compounds which had not been reported in literatures were synthesized and their structures were confirmed by ~1H-NMR and MS.