Upcoming Meeting
Wednesday, May 16, 2012
(formerly, The Crowne
Plaza Hotel)
Excellence
in Catalysis Award Lecture
Greg
Hughes
Merck
& Co.
Enabling
Technologies Lead
Process
Chemistry Department
Leveraging
Centers of Excellence in Catalysis and Analysis to Improve Pharmaceutical
Manufacturing
In
the past decade the Merck catalysis team has assembled world class capability
for the use of high throughput experimentation in the screening and
optimization of catalytic reactions. The
group pioneered many aspects of the use of microplate technology and laboratory
automation for modern catalysis research, introducing a number of the
instruments and techniques that are now commonly used in the field
today. More importantly, these
capabilities have profoundly impacted the way that new pharmaceuticals are
manufactured at Merck, with the development of a series of successful
catalysis-based commercial manufacturing processes . The Merck catalysis team's expertise spans
the traditional arena of catalysts for small molecule organic synthesis
research, but also includes substantial expertise in the development and
practical use of enzymatic catalysts.
The team also draws on a depth of expertise in laboratory automation and
high throughput analysis, both critically important to the successful practice
of modern high throughput catalysis research.
Several
examples will be presented to illustrate the important contributions of the
group to the field of catalysis. One of
the first clear-cut examples of the value of the high throughput catalysis
approach at Merck was the development of highly efficient and affordable
asymmetric hydrogenation routes for enantioselective synthesis of the drugs,
sitagliptin, ezetimibe, laropiprant, taranabant, suvorexant and MK-1597. Most recently, the group has collaborated
with Codexis on the directed evolution of improved enzymes to form highly
optimized catalysts for commercial manufacturing processes, delivering greatly
enhanced rate, specificity, and durability relative to the 'wild type' enzymes
from which they were derived. This work recently culminated in the
development of a substantially improved new enzymatic transaminase-based
manufacturing process for sitagliptin which will also be presented.
