Imatinib Synthetic Derivatives Nepal

Imatinib as the first targets tyrosine kinase BCR-ABL and has been demonstratedgood efficacy in treating chronic myloid leukemia clinically. However, with its widelyused in clinical application, a number of related issues, such as adverse reactions anddrug resistance appeared in succession. In recent years, more and more people focus ondeveloping new tyrosine kinase inhibitors.In this paper, the synthetic and process of Imatinib important intermediateN-(2-methyl-5-aminophenyl)-4-(3-pyridyl) pyrimidin-2-amine were investigated, andsome procedures were improved.2-methyl-5-nitroaniline and3-acetylpyridine wereselected as the starting materials. Then the final product was obtained in four stepsincluding nitration, addition, cyclization and reduction. Taking the product as basicstructure, for structural modification of the design, synthesis of phenoxy acetamide,urea, aroylthiourea derivatives including19imatinib derivatives. All these productshave been fully characterized by IR, MS and1H NMR.These compounds were tested of the inhibitory activity by the method of MTT. Theresults show that all of them have the inhibitory activity, and target F-7and G-5exhibited potent anticancer activity.