Diversity-oriented synthesis of natural product-like libraries

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.