Telmisartan New Synthetic Route Of The Study

Hypertension is an important risk factor for heart, brain and cardiovascular diseases that have seriously effect on the patients’life quality and become a primary cause of global deaths. Telmisartan is an angiotensin II receptor antagonist using in the treatment of hypertension and can smoothly reduce and steady the blood pressure. Furthermore, it has such advantages as long lasting, strong potency, safety, few side effects and high tolerance. It was first developed by Boehringer-Ingelheim in Germany and first available on the market of the United States as an antihypertensive drug with the brand name of MICARDIS in1999. Herein, looking for a new environment-friendly, cost effective and yield stable synthetic route for telmisartan is quite urgent and important for our society and economy.In this dissertation, we design and develop three non-infringing process for telmisartan starting from commercially available materials. Given an overall consideration of yield and cost, we finally choose method2as the efficient route for the industrial preparation of telmisartan. The subsequent laboratory optimization was performed and the synthetic process was successfully applied to prepare telmisartan in kg scale in42%overall yield. Also, the target product (Telmisartan1) and relevant intermediates were identified and confirmed by1H-NMR and MS.