| Fasudil hydrochloride is a new type of cardiovascular drugs, with a wide range of pharmacological effects. The chemical name of fasudil hydrochloride is hexahydro-1-(5-isoquinolinylsulfonyl)-1H-1,4-Diazepine hydrochloride, its molecular structure is 5- isoquinolinesulfonamide derivatives. As a kind of RHO kinase inhibitor is a new type Ca2+ antagonists in cell model, by increasing the activity of myosin light chain phosphatase (MLCP) to dilate the blood vessels, and reduce the tension of endothelial cells, effectively improve the microcirculation of the brain tissue, improve the subarachnoid hemorrhage (SAH) on the prognosis of the patients, does not produce and aggravate cerebral steal, at the same time reverse inflammatory cytokine, protect neural apoptosis, promote nerve regeneration. The drug has a huge market potential, optimizing the synthesis process and establishing the industrial production line and its quality control is a great significant.In this article, based on the process of literature and patent reports, based on the 5-Isoquinolinesulfonic acid as raw material, through acylation, chlorination, condensation, neutralization, extraction, separation, the process route of salt, finally get the fasudil hydrochloride,in the total yield of 52%. The product was conformed by UV, IR, NMR and elemental analysis, thermal analysis and other methods, to identify the structures of the synthesized compounds, the results showed that the structure of the compound was completely in conformity with that of the control substance.The quality of fasudil hydrochloride raw material drug control method in this paper is studied. Method for the determination of physical and chemical identification and content of impurities, is established according to the physical and chemical properties and structure characteristics of the product. Related substances by TLC method. Provide analysis method is accurate and feasible for the study of fasudil hydrochloride raw material quality control. |
PDF Full Text Request