Plenary Session, Award- or Invited Lecture
The Importance of Catalysis in the Synthesis of Active Pharmaceutical Intermediates (KGF-SCS Senior Industrial Science Award Lecture 2015)
M. Scalone1
1F. Hoffmann-La Roche AG, Pharmaceuticals Division, Process Research & Development, CH-4070 Basel, Switzerland
In recent years, a clear tendency towards increasing structural and stereochemical complexity of new drug candidates is observed. This factor, together with the limited amount of time and resources available to invent and develop more efficient syntheses, often lead to a critical issue regarding cost of the active pharmaceutical ingredient (API).

This presentation will illustrate how the early integration of catalysis in the synthesis plan of three new development compounds has not only been the condition to guarantee the timely supply of the amounts required for the planned preclinical and clinical investigations, but has also set the base for scalable and economical synthetic processes. Four reactions will be discussed as an example, three based on metal catalysis (carbonylation, asymmetric hydrogenation, ring-closing metathesis) and one on enzymatic catalysis (asymmetric keto reduction).