Buchwald wins Siegfried Medal from University of Zurich
The University of Zurich and Siegfried Ltd announced that Professor Stephen L. Buchwald of Massachusetts Institute of Technology will receive the 2006 Siegfried Medal for his achievements in process chemistry. Professor Buchwald's contributions have effected process chemistry primarily in the synthesis of fine chemicals and active pharmaceutical ingredients, with specific achievements including:
1) Design of commercially viable ligand systems to facilitate metal mediated coupling reactions
2) Elaboration of robust synthetic protocols applicable to target synthesis on scale
3) Evaluation of reaction mechanisms to minimize catalysts loadings leading to more environmentally safe chemical processes.
In the area of ligand design, Buchwald is well known for the family of now commercially available biaryl phosphines, which he has used to demonstrate substrate/reactant generality in coupling reactions ranging from arylboronates and arylchlorides in the classic Suzuki-Miyaura reaction to ketones and nitroarylhalides in the synthesis of pharmaceutically important indoles. This ligand mediated chemistry has been used on scale by major pharmaceutical companies; one particular example being the antidepressant MKC-242. The use of metals on scale is only possible if cost, safety and environmental issues can be resolved through mechanistic considerations, Buchwald has been able to optimize these processes to require low catalysts loadings, to be less sensitive to conditions, and to work safely and reliably. This spectrum of achievements from fundamental reaction design to optimized commercially robust process embodies API process chemistry.
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