Chemical synthesis is one of the key technologies underlying modern drug discovery and development. For the design and accessibility of novel structures and the rapid preparation of new test compounds and development candidates with often highly complex chemical architecture, it is essential to use state-of-the-art chemical synthesis technologies. Recent developments in the field of asymmetric catalysis point to a third class of catalysts besides the established enzymes and metal complexes, so-called organocatalysts. These low-molecular-weight, organic molecules enable highly chemo- and stereoselective chemical transformations for the rapid assembly of complex bioactive molecules of interest for the pharmaceutical industry. This book presents the contributions from leading experts, with backgrounds in academia and industry, to an Ernst Schering Research Foundation Symposium held in April 2007. It illustrates current progress in organocatalysis in functional group interconversions, organocatalytic CC- and CX-bond formations with small molecules as well as peptide-based catalysts and genetically engineered enzymes and their applications in natural product and drug syntheses. It will be of interest to those who want a general overview of the topic, but also to those who want to learn more about the state of the art, current trends and perspectives in this highly dynamic field of research.