肿瘤相关糖抗原GM3及其衍生物合成方法研究进展  

Research progress in the synthesis of tumor-associated carbohydrate antigens (TACAs) GM3 and derivatives

作　　者：白国静[1,2] 边晓杰[2] 姚阔 吴俊琪[2] 俞世冲[2] 孟庆国[1] 吴秋业[1,2] 

机构地区：[1]烟台大学药学院,山东烟台264005 [2]第二军医大学药学院,上海200433

出　　处：《药学实践杂志》2016年第1期5-7,15,共4页Journal of Pharmaceutical Practice

基　　金：国家自然科学基金青年项目(21202200);国家科技部重大专项重大新药创制(2012ZX09502001-005);第二军医大学本科生创新基金项目

摘　　要：GM3及其衍生物合成中的糖苷化反应条件苛刻,端基碳的立体构型较难控制,能否高效地得到α糖苷键是评价反应优劣的重要标志之一。笔者综述了近年来GM3及其衍生物的合成方法,涉及糖供体化合物的选择、糖受体的确定、立体选择性的控制及新糖苷化反应催化剂的发展。Glycosylation is the key step of the synthesis of GM3, its reaction conditions are very harsh, the stereoselec- tivities are usually poor, and the configuration of anomeric carbon is difficult to control. Whether α glycosidic bond can be con- structed efficiently in sialylation reactions is an important criteria used to evaluate the reaction quality. Studies of GM3 and de- rivatives methods generally relates to following areas： the choice of the donor compounds and receptor compounds, the control of stereoselectivity, and the development of some new glycosidic reaction catalyst. In recent years, important progress has been made in this research area. Now, we predominately make a summary and review on the progress of methods for the synthesis of GM3 and derivatives.

关 键 词：GM3及其衍生物 合成 糖供体 糖受体 糖苷化反应 立体选择性 

分 类 号：R914.5[医药卫生—药物化学]