中文摘要：

天然产物是药物发现中先导化合物的重要来源.高通量筛选技术的发展和近年来化学生物学研究的深入,对拓展天然产物与活性相关的＂化学空间＂提出了新要求.用多样性导向合成方法建立骨架多样、构造复杂、立体化学多样性的＂类天然产物＂化合物库进行生物学相关研究,并以此为基础发现药物先导化合物正在成为一种趋势.在此过程中,发展具有立体选择性和区域选择性,能够广泛应用于多种底物的有机化学反应起着关键作用.

英文摘要：

Natural products provide the most important sources of lead compounds in drug discovery. With the development of high-throughput screening （HTS） technology and in depth studies in chemical biology, exploring pharmaceutically relevant chemical space of natural products is vital. Employing diversity-oriented synthesis （DOS） to construct skeletally complex natural product-like libraries and using it in the studies of chemical biology and lead discovery is becoming a tendency. The development of exceptionally efficient, stereoselective, and chemoselective reactions that can be applied to a wide range of substrates play key roles.