Research On Synthesis Optimization Of Dasatinib

At present the focus of anticancer drug is moving from traditional cytotoxic drugs to new anticancer drugs, targeting tumor cells transduction pathway of signal. Tyrosine protein kinases has been shown to induce a wide variety of tumor cells by several mechanisms mainly including exerting important modulatory effection the proliferation, differentiation, migration and metabolism-related signal transduction pathways in cells. Tyrosine kinase inhibitor has been developed as a new kind of antitumor drug in recent years, and dasatinib is a representative drug of Tyrosine inhibitor in clinic. This article summarized the research progresses on chronic myeloid leukemia (CML) and Tyrosine kinase inhibitor, especially mechanism of action and the research progresses on the clinic of dasatinib. Nowadays, there are not many reports for the synthesis of dasatinib. On the basis of literature of the three synthetic routes, with environmentally friendly, less reaction steps, simple, safe operation, the yield rate and satisfy the principle of large-scale production.N-(2-Chloro-6-methylphenyl)-2-[(6-chloro-2-methyl-4-pyrimidinyl)amino]-5-thia zolecarboxamide was synthesized by condensation between N-(2-Chloro-6-methylphenyl)-2-[(6-chloro-2-methyl-4-pyrimidinyl)amino]-5-thiazole carboxamide and N-(2-Hydroxyethyl) piperazine. We hope to get one method which is more economical, yield is higher, pollution is lower, conduction is easier and suitable for its industrialized production. The reaction yield was77.80%, and the purity of the product reached99.89%All products were characterized by modern analytical methods including UV, IR, HNMR and MS, and their structures are assured.