Selpercatinib is a rearranged during transfection(RET)tyrosine kinase inhibitor with high selectivity,and is the first approved targeted drug specifically for cancer patients with RET gene mutations in the world.This article reviews the synthetic routes of selpercatinib and its intermediates,and makes a comparative analysis of seven synthetic routes of selpercatinib,and compares the yield,process hazards,and industrial feasibility.It is proposed that the three synthetic routes starting from 3-bromo-5-mrthoxypyridine,3,5-dibromopyridine and 3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-3-azabicyclo[3.1.1]heptane-6-carboxylate respectively are more suitable for industrial production.Compared with the other four synthetic routes,these three synthetic routes have the advantages of available raw materials,simple operation,high yield and low cost.
selpercatinibrearranged during transfection tyrosine kinase inhibitorsynthetic routetargeted drug
万方数据
维普
