碳青霉烯和青霉烯类抗生素的固相全合成

We have first developed a solid-phase synthetical methodology of carbapenems using cross-link polymer PS-DES-SiCl resin as support. This method possesses several advantages such as higher yield, facile operation and generality, and, therefore, could be used in the combinatorial chemistry. A small carbapenem-based library has been prepared by this method. We also developed new polymer-supported methods for the synthesis of some other heterocycles including isoxazoles, 1, 2, 4-oxdiazoles, 3, 4-dihydro- pyrimidin-2(H)-ones as well as indoles. These results could be used in the combinatorial chemistry and parallel synthetical techniques.

本项目拟研究经由同一固相手性砌块来合成结构不同的碳青霉素烯和青霉烯类抗生素的固相不对称全合成方法,并利用该方法合成一个小规模化合物库.通过研究,建立一种高效,简便,哂型ㄓ眯缘奶记饷瓜┖颓嗝瓜├嗷衔锖铣尚路椒?发现一批具有抗菌活性的新化合物,同蔽米楹匣Ч菇ɑ衔锟?大规模筛选抗生素提供重要的方法学依据.