Synthesis Research Of Intermediate Of DPP-? Inhibitor-saxagliptin,synthesis And Structural Characterization Of Rosiglitazone Derivative

Over the years,the attention of Saxagliptin,an important drug for the treatment of diabetes,has remained high both at home and abroad.For the synthesis of Saxagliptin,3-hydroxy-1-acetyladamantane is an important intermediate in the synthesis of Saxagliptin.Through literature review of its related synthetic routes,it is known that there are five main synthetic routes.The synthetic route with higher yield was improved.3-hydroxy-1-acetyladamantane was synthesized from adamantanecarboxylic acid by thionylchloride acylation,NCS added in,substitution by diethylmalonate,decarboxylation,alkalization respectivly.The overall yield was about 70%.Compared with the original route,the improved route reduced the hydroxylation reaction of mixed acid,and the total reaction step was reduced from 5 to 4 steps,which shortened the reaction time.At the same time,on the premise of guaranteeing the yield,the reaction efficiency is improved,making it more suitable for industrial production.In addition,based on the research results of Rosiglitazone derivatives,the structure modification of Rosiglitazone was continued.Eight related compounds from RSG-1 to RSG-8 were synthesized,and their structures were characterized.The related compounds with certain anticancer activity were preliminarily screened out.