Synthesis And Quality Study On Imatinib Mesylate

Being plagued by cancer, cardiovascular and other non-communicable diseases, people graduallydevelop the appropriate drug for these diseases under the help of the continuous development of thetechnology. Chronic myelogenous leukemia (CML), belongs to the diseases caused by the hematopoieticstem cell cloning of malignant hyperplastic, the incidence in our country is about3.6percen. The latestresearch and development of molecular targeted therapy is imatinib mesylate. It is a tyrosine kinaseinhibitor (IXI) and has already achieved good results now.This paper first summarizes the research status of the tumor, which including the introduction, symptoms,the triggers, and the comparison of conventional and modern treatment methods. And then some tyrosinekinase inhibitor drugs were put forword. Some research progress of imatinib mesylate is concluded, suchas the development, phase III clinical trials, pharmacokinetics, pharmacological action, clinical indicationsand adverse reactions and so on. The theme part of this paper briefly describes the synthesis of imatinibmesylate. On the basis of previous research work, the following synthetic route is designed. With thestarting material of imatinib amines, N-methyl piperazine and4-chlormethyl-benzoyl chloride, afterseveral condensation reactions, the beta crystal type of imatinib mesylate is finally synthesized. Thesynthetic routes are optimized through lots of experiment and finally the appropriate reaction solvent,reaction temperature and crystallization method are selected. As a result, the reaction route is both easy andeconomically environmental. The structure of the target compounds were characterized by HPLC-MS,1HNMR and other analytical tools. The results showed that the experimental products were consistent withthe objective product and the structural characterization and performance are consistent with the requirements of the experiment goal. The total reaction yield is relatively high, and there is no columnseparation process, post processing is simple, suitable for industrial production. Mild reaction conditionmakes the process controllable and the final product is beautiful white crystal.On the basis of the synthesis of the final product, imatinib mesylate quality research work is proceed,which is mainly on its physical and chemical properties, examine, content and other projects. Initiallyidentified associated quality control method provides the basis for the expansion of production for future.