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Organocatalysis
Berlin ; New York : Springer, ©2008.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.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.".
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