Chemical synthesis is one of the key technologies that form the basis of modern drug discovery and development. For the rapid preparation of new test compounds and the development of candidates with often highly complex chemical structures, it is essential to use state-of-t- art chemical synthesis technologies. Due to the increasing number of chiral drugs in the pipeline, asymmetric synthesis and ef?cient chiral separation technologies are steadily gaining in importance. Recently a third class of catalysts, besides the established enzymes and metal complexes, has been added to the tool kit of catalytic asymmetric s- thesis: organocatalysts, small organic molecules in which a metal is not part of the active principle. Despiteconsiderable effortstoexploreand extend thescopeofas- metric organocatalytic reactions in recent years, their use in medicinal and process chemistry is still rather low. This is even more surpr- ing as the ?eld was pioneered by the medicinal chemistry laboratories of Schering AG and Hoffmann La Roche in the late 1960s and early 1970s by using proline as asymmetric catalyst in a Robinson annulation to obtain steroid CD ring fragments, a process now referred to as the Hajos–Parrish–Eder–Sauer–Wiechert reaction. Inanefforttoincreasetheawarenesswithinthecommunityofmed- inal and process chemists, and to learn more about recent progress in this rapidly evolving ?eld, the Ernst Schering Foundation enabled us to VI Preface organize a symposium on ‘Organocatalysis,’ which took place in Berlin, Germany, from18to 20 April2007. Theproceedings ofthis symposium are detailed in this book.
Excellent overview on state of the art of modern organocatalysis