Process Improvement Of Trbesartan And Synthesis Of Its Berivatives

Hypertension is the most common cardiovascular disease,which is also one of the risk factors to coronary heart disease,stroke,renal dysfunction.The treatment of hypertension can not only reduce blood pressure,but also protect the brain,heart,kidney and other target organs.At present,many domestic and foreign data show that angiotensin II receptor antagonists can improve the prognosis of patients with long-term hypertension,and reduce the mortality and the incidence of stroke,heart failure and cardiovascular events.Therefore,it is important to develop better curative effect of angiotensin II receptor antagonists.In the paper,the synthesis route of Trbesartan is optimized by changing the feeding rate and reaction time,finally,I can achieve the hektogram level of Trbesartan,its R and its S,the purity of which reach more than 99%.in the process of purification,the paper use recrystallization instead of column chromatography,which greatly improve the production efficiency.when I made them into the form of potassium,they have the better effect of oral antihypertensive,at the dose of 10mg/kg,Trbesartan potassium is similar to losartan potassium in the antihypertensive effect,in vitro tumor cell growth inhibition test,Trbesartan potassium shows a good primary inhibitory rate for HCT-8 human colon cancer cell lines.Discovered from molecular docking model from this research group,.there is a distinct space between the side chains of benzimidazole and the receptor,therefore,it is possible that Trbesartan have insufficient length in the 2-carbon chain of benzimidazole,Theoretically,The closer the drugs bind to the receptor,the better the effect will be,we shorten and lengthen the 2-carbon chains of benzimidazole in this paper,new target compound was synthesized by introducing methyl,ethyl,n-Bu,n-pentyl respectively.