The Research Of Antibacterial Quinolones And Oxazolidines

Quinolones and oxazolidines are two kinds of important synthetic antibacterial drugs,which are widely used in clinical trials and have made great contribution to human heath.Take into the actual situation of china’s pharmaceutical research,the "me-too" drug research strategy is more practical,so we have carried on some structural modification of quinolones and oxazolidines.This dissertation includes the fllowing two parts.The part one is the study of quinolones.In this part studied synthesis of side chains and quinolone nuclear parents were respectively.At first four side chains were obtained by using amino acids as the starting materials via esterification,acetylation,cyclization,reduction,protection and debenzylation.Then three quinolone nuclear parents were obtained by using 2,4,5-trifluoro-3-methoxy-benzoic acid and ethyl 3-oxo-3-(2,3,4,5-tetrafluorophenyl)propanoate as the starting materials respectively.Design and synthesis of 18 quinolones compounds.At last the side chains and quinolone nuclear parents were connected by microwave reaction to short the reaction time and improve the reaction efficency.The chemical structures of target compounds and important intermediates were confirmed by NMR,HRMS.The results of in vitro antibacterial activity tests show that most of target quinolone analogs have good activity.Especially STM-5 and STM-6 have better activity than ciprofloxacin and similar to levofloxacin.In second part,the synthesis of analog derivative of linizolid,an oxazolidine antibacterial drug was investigated.We have designed and developed a novel route to synthesize oxazolidines.The target molecular EZ5-10 are successfully achieved by using 2-amino-2-methylpropan-1-ol as the starting material via acetylation,oxidation,Henry reaction,protection,oxidation,reductive amination,deprotection and cyclizati-on.Thus we found a possible route to modify the E area of oxazolidines with cheap raw materials,mild reaction condition and simple operation.