Synthesis And Cytotoxic Activity Of ?-lactam Spiro Compounds

?-lactam compounds and aza-spiro compounds have become the focus and hotspots of pharmaceuticals,pesticides and chemists due to their significant antibacterial activity and extensive biological activity,and the aza-spiro compounds have non-spiro compounds of the drug resistance,low side effects,the impact on the environment and other excellent.These compounds have made great contributions to human health and scientific research and have important research value.Based on the excellent bioactivity and properties of the?-lactam compounds and the aza-spiro compounds,we envision the design of the pharmacophore P-lactam ring and the aza-spiro ring structure in the same drug molecule to look for screening with low resistance,good selectivity and low toxicity of P-lactam spiro compound.This paper mainly using the oxidative dearmatization with IBD,construction of spiro rings by tandem carbon carbon bond,introducing all kinds of primary amine,the synthesis of novel structure and exhibited inhibitory activity ?-lactam spiro compounds.This paper is divided into four chapters,the first chapter mainly summarizes antibacterial activities,biological activities and synthetic methods of ?-lactam compounds.Synthetic methods mainly include including Staudinger reaction,Kinugasa reaction,cyclization reaction and other synthesis methods of beta lactam compounds has significant antibacterial activity,found in recent years also has anti-cancer,anti malarial,central nervous system and active agent,inhibiting human virus,cytomegalovirus protease serine protease inhibition and cholesterol absorption inhibitor activity.The second chapter mainly introduces the various synthesis methods of aza-spiro compounds,including oxidation to aromatization,intramolecular and intermolecular cyclization,meta-catalyzed,and aza-spiro compounds in medicine and pesticide application are briefly introduced.The third chapter introduces adoption of catalytic amount of copper salt,IBD oxidative dearmatization method,exploring on the ?-lactam skeleton introduced all kinds of primary amine.35 ?-lactam compounds,containing spiro structure,were synthesized,and these compounds were evaluated in vitro against a panel of human tumor cell lines.The fourth chapter are the experimental operation and compound spectra data.