The Basics of Diversity-oriented Synthesis

In this chapter, the underlying ideas behind diversity-oriented synthesis are introduced. The relationship between diversity-oriented synthesis and combinatorial chemistry is discussed, and the rationale behind the use of diversity-oriented synthesis as a tool for the discovery of biologically active molecules is explained. Common synthetic strategies for the efficient generation of structurally diverse compound collections are then introduced. In the second part of the chapter we discuss recent examples of diversity-oriented syntheses, with examples taken from our own research and from the wider community. These examples seek to illustrate the imaginative ways in which the various synthetic strategies have been implemented and to represent the current state of the art in diversity-oriented synthesis.