Preface
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-theart chemical synthesis technologies. Due to the increasing number of
chiral drugs in the pipeline, asymmetric synthesis and efficient 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 synthesis: organocatalysts, small organic molecules in which a metal is not
part of the active principle.
Despite considerable efforts to explore and extend the scope of asymmetric organocatalytic reactions in recent years, their use in medicinal
and process chemistry is still rather low. This is even more surprising as the field 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.
In an effort to increase the awareness within the community of medicinal and process chemists, and to learn more about recent progress in
this rapidly evolving field, the Ernst Schering Foundation enabled us to
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-theart chemical synthesis technologies. Due to the increasing number of
chiral drugs in the pipeline, asymmetric synthesis and efficient 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 synthesis: organocatalysts, small organic molecules in which a metal is not
part of the active principle.
Despite considerable efforts to explore and extend the scope of asymmetric organocatalytic reactions in recent years, their use in medicinal
and process chemistry is still rather low. This is even more surprising as the field 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.
In an effort to increase the awareness within the community of medicinal and process chemists, and to learn more about recent progress in
this rapidly evolving field, the Ernst Schering Foundation enabled us to