A method with safety and convenience to synthesize Regorafenib

Abstract

To date, three methods have been developed to synthesize Regorafenib, a drug which can effectively cure colorectal cancer. However, all of them have drawbacks: some are complicated to obtain due to the high requirements the drugs need. And some even contain dangerous processes or poisonous drugs that are difficult to store. Also, there is a way that contains a lot of by-products, which makes extracting Regorafenib very difficult. In this essay, one of the synthetic routes and the data from the experiment will be used to test whether it works. Furthermore, the selected route was improved. Here, the best base on the reaction is t-BuOK; 1.1 eq of potassium tert-butoxide was preferred; the most appropriate temperature is 100°C; the ZA1 and SM3 feeding ratio is preferably 1.10 eq; the reaction time can be chosen 3-7 h.