Due to the emergence of organocatalysis as a highly active and very exciting field of research both in academia and the life sciences industry, an Ernst Schering Research Foundation Symposium was organized in 2007 to bring together the scientific leaders in this field and to discuss the basics and current progress of organocatalysis and its application in drug discovery. Various aspects of organocatalysis are addressed in this volume, covering a broad range of synthetic transformations such as functional group interconversions as well as CC- and CX-bond formations and their applications in natural product and drug syntheses. In addition, the design and scope of various catalyst systems are discussed, from small molecules, to peptides, to genetically engineered enzymes.