Studies On The New Synthesis Of Betrixaban

Thromboembolism as the 21 st century’s biggest disease is serious harm to people’s health,which has become the main cause of death and disability.It can involve to every organ and system in our body,and it has the characteristics of high incidence,morbidity and mortality.On average,every year about 3 ‰ of the people occur different types of thrombotic diseases,it has been a serious threat to human health.Our country has more than 3 million people die each year from disease of heart head blood-vessel.Anticoagulation in thromboembolic disease treatment occupies an important position.Serine protease factor Xa plays a pivotal role in the blood coagulation cascade.Factor Xa inhibitors by extending clotting process,reducing the generation of thrombin realize the anticoagulant effect,and they are selective to factor Xa.Xa factor as the targets of anticoagulant drugs appeared continuously.In this paper,on the basis of the traditional a few of synthetic routes,we design and develop a new simple method of synthesis of Betrixiban.The new synthetic route ably avoided dechlorination impurity.By optimization of the reaction process,the final product betrixiban(the purity is 99.7%,and total yield is 47 %)was obtained.And the final product and reaction intermediates was confirmed structural characterizationusing using high performance liquid chromatography(HPLC),infrared absorption spectroscopy,nuclear magnetic resonance hydrogen spectrum,carbon nuclear magnetic resonance spectrum and mass spectrum and so on.At the same time,the preliminary quality of the final product was carried on.Finally,through the study of design route and optimization,we carry out a synthetic rout which has simple operation,easy control of reaction process,high yield,high product purity,cheap reagents,less reaction waste and suitable for industrialized production advantages.