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Synthesis Of β - Lactam Spiro Compounds And Their Asymmetric Synthesis

Posted on:2016-11-27Degree:MasterType:Thesis
Country:ChinaCandidate:Z H JinFull Text:PDF
GTID:2271330470455281Subject:Pharmaceutical Engineering
Abstract/Summary:PDF Full Text Request
β-lactam has be paid much attention due to strong antibacterial activity of peniciiiin had be found by Fleming. More and more studies have been carried out about β-lactams because of the wide-ranging application of penicillin and cephalosporins.As the core skeleton and antibacterial groups of β-lactam antibiotics, β-lactam has long been a study object of pharmacologists and organic chemists. Recently, the focus of the research is to enhance the stability of β-lactam ring and modify nucleus structure of peniciiiin for developing the new antibiotics. Besides being the core skeleton of antibiotic, other pharmacological activities such as cholesterol inhibitors, β-lactamase inhibitors and so on had been found. This thesis describes an approach to construct the spiro-p-lactam using the oxidative dearomatization with IBD.This paper is divided into three chapters, the first chapter summarizes the history of the β-lactam, the structural transformation of cephalosporin C, the use of carbapenems, the other use of β-lactam, the antibacterial mechanism and resistance mechanisms of β-lactam antibiotics, a brief introduction the main synthesis of β-lactam, for example [2+2] cycloaddition, Intramolecular addition, the inset of CO, and the strcuture of four-membered ring β-lactam.The second chapter study the introducing of the different amino acid and the construction of the chira carbon in the spiro-β-lactam.The third chapter introduces the expermental operation and suportinformation.
Keywords/Search Tags:β-lactam, Trost, chiral spiro
PDF Full Text Request
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