ACS ProSpectives Conferences on the Discovery, Development & Production of Pharmaceuticals and Therapeutics

Organic Reactions & Syntheses

October 26 – 28, 2008 | The Hyatt Regency Penn’s Landing | Philadelphia, PA

Overview

Due to popular demand for a conference dedicated solely to “hardcore” organic synthesis, conference chairs Nick Magnus, Research Advisor in process research at Eli Lilly, and Mo Movassaghi, Associate Professor of Chemistry at MIT, invited both academic and industrial speakers to present chemistry in the areas of catalysis, heterocyclic chemistry, asymmetric synthesis, methodology, and total synthesis. The conference explored strategies that enable the preparation of new pharmaceutical agents, molecular probes, complex natural products, and organic materials.

Speakers from major pharmaceutical companies presented case studies that detail the techniques they employed to solve synthesis problems to enable the clinical evaluation of new medicines.

Speakers and Topics:

Rob Waltermire, Group Director Chemistry Technologies, Bristol-Myers Squibb

• Practical Asymmetric Synthesis of Drug Candidates at Bristol-Myers Squibb Process R&D

Greg Fu, Firmenich Professor of Chemistry at MIT

• Palladium- and Nickel-Catalyzed Coupling Reactions

André Charrette, Professor at the the Université de Montréal

• Transition Metal Catalyzed Asymmetric Cyclopropanation of Alkenes with Diazo Reagents Bearing Two Electro-withdrawing Groups

Andreas Pfaltz of Univ. of Basel

• Iridium-Catalyzed Asymmetric Hydrogenation

Jan-Erling Bäckvall , Professor at the University of Stockholm

• Recent Advances in the Combination of Metal and Enzyme Catalysis

Andy Wells, Principal Scientist, Global Process R&D, AstraZeneca

• Global Process R&D: Some Applications of Biocatalysis in the Synthesis of Pharmaceutical Intermediates

Tomislav Rovis of Colorado State

• Catalytic Asymmetric C-C and C-N Bond-Forming Reactions

Amos B. Smith III, Rhodes-Thompson Professor of Chemistry, Penn

• Multi-Component Anion Relay Chemistry (ARC): A Useful Tactic for the Construction of Architecturally Complex Natural and Unnatural Products

Joel Hawkins, Senior Research Fellow, Pfizer

• Case Studies in Pharmaceutical Process R&D involving Batch and Flow Chemistry

Nathan Yee, Boehringer Ingelheim

• Scale-Up of Ring-Closing Metathesis Reaction: Development of a Highly Practical Process for Macrocyclic HCV Protease Inhibitors

Tony Zhang, Managing Director, Eli Lilly Research Labs, China

• Process Development of Polyaromatic Drug Candidates

Francis C. Fang of Eisai

• Process Research on Natural Product Drug Candidates: Halichondrin Analog E7389 (Eribulin)

Michael J. Krische, Director, Center for Green Chemistry and Catalysis, Univ of Texas

• Formation of C-C Bonds via Catalytic Hydrogenation and Transfer Hydrogenation

Karen Sutherland of Wyeth

• The Development of a Manufacturing Process for a Late Stage HER-2 Inhibitor

Jeffrey Moore of Merck

• The Future of Biocatalysis in Big Pharma: Target ID Through Process Development

The optional full-day short course was offered on Sunday before the conference. Professor Peter Jacobi of Dartmouth taught on heterocyclic chemistry in the morning, and Horacio Olivo of the Univ of Iowa, taught on bio-transformation in the afternoon.