Conference chairs Pat Confalone of DuPont and Joseph Fortunak of Howard University developed the 2008 program for the “Process Chemistry in the Pharmaceutical Industry” conference with an emphasis on process R&D and a look into how another industry navigates the issues of commercial ramp up and manufacturing.
A number of case studies from the pharmaceutical industry were given to highlight the challenges and rewards of discovering and developing commercial manufacturing processes for novel therapeutics. The engineering aspects of process R&D, including kinetics, process parameters, process analytical technology, and green chemistry, were also explored.
A half-day was devoted to presentations from the crop protection sector, where cost of goods is a critical success factor, and practitioners must develop commercial processes within severe cost constraints in the face of complex active ingredient targets. This requires highly convergent syntheses with starting material pricing less than $ 10 / kg, often eliminating several excellent alternative routes for the manufacturing process. Many of the insights from the Agrichemicals industry proved beneficial to pharmaceutical Process R&D organizations.
Though the focus of the conference was on process chemistry currently in practice in industry, as always, noted academics presented their ideas and work on important novel methodologies that will impact process R&D capabilities in the near future.
A full-day short course was given on Sunday, Sept. 28, from 8:30 AM – 5 PM with lunch included. In the morning, Peter Jacobi of Dartmouth instructed on heterocyclic chemistry, and in the afternoon, Dave Collum of Cornell taught reaction kinetics.
PROGRAM
Recent Advances from Academia
Scott Denmark, R. C. Fuson Professor of Chemistry at the University of Illinois
Victor Snieckus , Professor at Queen’s University
• Regioselective Synthetic Processes Based on the Aromatic Directed Metalation Strategy
Gary Molander, Hirschmann-Makineni Professor at Penn
• Organotrifluoroborates in Suzuki Coupling
Steve Martin of the University of Texas
• Recent Advances in the Synthesis of Heterocyclic Natural Products
Pharmaceutical Process R&D I
Sebastien Caille of Amgen
• Asymmetric Approaches to Chiral C-5 Dialkyl Substituted 2-Aminothiazolones
Rodney L. Parsons , Group Director, Process Research and Development at BMS
• From Lab to Plant, Process Research and Development for a Statin Drug Candidate
John Ragan of Pfizer
• Development of Synthetic Routes for the Preparation of Two CB-1 Antagonists for Treatment of Obesity."
Steven J. Coote of GlaxoSmithKline
• A Case Study on the Development of a Commercial Manufacturing Route for Veramyst (Fluticasone Furoate)
Process R&D in Crop Protection Chemicals
Rafael Shapiro of Dupont
• The Evolution of a Manufacturing Process for RynaxypyrTM
Mark Ford, Head of Process Research Frankfurt, Bayer CropScience
Bill Rigby, Manager of Process Technology, Syngenta
Douglas Bland, Research Specialist, Dow
• Overview of Process Route Developments Leading to the Manufacture of Pyroxsulam
Pharmaceutical Process R&D II
David Askin, Sr. Scientific Director, Merck Research Labs
• From Crixivan® to Isentress®: Process Research Innovation on Merck’s HIV Franchise
Jerry Salan of Pfizer
• Process Design and Modeling in Pharmaceutical Development of APIs
Jesper Jernelius and James Davidson of Roche Palo Alto
• Process Development of Non-Nucleoside Inhibitors of HIV Reverse-Transcriptase (nNRTIs)
Nathan Yee, Boehringer-Ingelheim
• Development of Highly Practical Large Scale Ring-Closuring Metathesis for Macrocyclic HCV Protease Inhibitors