单一糖缀化合物的大量获取，一直是制约着糖科学研究的瓶颈。而如何提高糖苷化的普遍适用性和效率，则是这其中的关键问题。本课题将在本小组发展的金催化炔酯给体糖苷化方法的基础上，对此方法进行突破性优化升级，大幅度提升催化效率，并实现该糖苷化方法的普遍适用性，建立例如1，2-顺式，2-脱氧等特殊糖苷键的一般性构建方法，解决这一长期困扰糖化学领域的核心问题。在此基础上，我们将完成bradyrhizose, 杠柳甙(periploside) A和axinelloside A这三个极为复杂的天然活性糖缀物的全合成，使之成为糖化学界的标志性工作。

Access to various homogeneous glycans and glycoconjugates in large amounts is still a bottleneck in the field of glycosciences. A key problem is to enhance the efficiency in construction of the extremely diverse glycosidic linkages. This project is based on our recent invention of a groundbreaking new glycosylation protocol, in that an unprecedented activation mechanism with glycosyl ortho-alkynylbenzoates as donors and a gold(I) complex as catalyst is employed. Further upgrading this protocol would establish a general and powerful method for glycosylation, so as to solve the long-lasting problems such as the constructions of 1,2-cis- and 2-deoxyglycosidic linkages. Applying the new methods, the total synthesis of several representative complex glycans and glycoconjugates of potent biological activities, including bradyrhizose, periploside A, and axinelloside A, will be tackled. The accomplishment of the total synthesis of these novel and extremely complex molecules would represent milestones in the synthetic carbohydrate chemistry.