Design And Synthesis Of 6-phenyl-imidazo [1,2-a] Pyridine-2-carboxamide Derivative

Cancer is one of the the most serious medical care problems in the word,that poses a great threat to human health.Because the cytotoxic characteristics of anti-cancer drugs,the human body has suffer many side effects.Therefore,the molecular targeted drug is expected to become an effective means of treatment.Many studies have revealed that the abnormal activation of intracellular signaling pathways are related to the tumors.An example of this would be the contribution of abnormal activation of the hedgehog(Hh)signaling pathway in a variety of cancer types.Sonidegib a new medicine which used to treatment of basal cell carcinoma develpoed by Novartis.It is can achieve remedial goal by by inhibiting Smo protein in the Hh signaling pathway.In this project,two types of compounds with imidazo[1,2-a]pyridine as the nucleus were designed,and to determine its synthetic route.The Series A compounds retain the pyridine:starting from 2-Amino-5-bromopyridine,two compounds were synthesized by cyclization,Suzuki reaction,hydrolytic reaction,amidation reaction.The Series B compounds change pyridine into benzene:starting from 2-amino-5-bromopyridine,eighteen compounds were synthesized by same way.Total 20 new compounds,which had not been reported,were characterized and confirmed by MS and1H NMR.The reaction conditions were optimized and the overall yield of the reaction is 23?30%.