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Day 1
Monday, October 24
7:30 Registration and Morning Coffee
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Process Chemistry in the 21st Century: Session I
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8:20 Chairperson's Opening Remarks
Dr. John DeMattei, Senior Group Leader, Process Chemistry, Array Biopharma
8:30 Optimization and Scale-Up of a Room Temperature Fu Suzuki Reaction
Dr. Christopher R. Schmid, Chemical Product Research & Development, Eli Lilly and Company, Lilly Corporate Center
The Fu Suzuki reaction, a room-temperature variant of the classic Suzuki coupling reaction using P(t-Bu)3 and a palladium source, was employed for the key carbon-carbon bond forming step in the kilogram-scale preparation of a clinical candidate. Reaction enablement, optimization, general and substrate-specific scope and limitations, and other findings encountered while implementing this methodology on kilogram scale will be presented.
9:00 Preparation of Pyrrolidine Based PDE-IV Inhibitors
Dr. John DeMattei, Senior Group Leader, Process Chemistry, Array BioPharma
This talk will demonstrate the development of a catalytic enantioselective conjugate addition/diastereoselective reductive cyclization to prepare quaternary carbon centers with asymmetric control. This methodology was then applied to the synthesis of PDE-IV inhibitors.
9:30 An Efficient Asymmetric Synthesis of a Selective Estrogen Receptor Modulator
Dr. Z. Jake Song, Senior Investigator, Process Research, Merck & Co., Inc.
A scaleable, asymmetric synthesis of a selective estrogen receptor modulator (SERM) that features a novel, unprecedented chiral sulfoxide directed borane reduction of cyclic vinyl sulfoxide will be presented. Investigation into the mechanism of this novel reduction will also be discussed.
10:00 Coffee Break
10:30 Process Development of (S)-Cyclohexylphenyl Glycolic Acid
Dr. Nandkumar Bhongle, Principal Research Chemist, Chemical & Pharmaceutical Sciences, Sepracor Inc.
This proposal includes work that involves a majority of the aspects of the pharmaceutical chemical process development. This asymmetric process is a demonstration of Seebach's concept of self-regeneration of stereochemistry at pilot scale.
10:45 Technology Watch (Sponsorship Available)
11:00 Roundtable Discussion Topics
• Dealing with transition metal contamination and impurities
strategies and regulatory consequences
• The challenges in integrating process analytical technologies into a
GMP environment
• The incorporation of automation technologies into the research
environment of process chemistry
• The natural interface of "green chemistry" and process
chemistry/Coping with increased regulatory stress from the FDA
• Approaches to the handling of high potency compounds |
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Moving Toward a “Greener” Future
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12:00 Sustainable Materials Design
Dr. John Warner, Professor, Director of University of Massachusetts Lowell Center for Green Chemistry
Recent developments in materials design have demonstrated that environmentally benign synthetic alternatives are not only possible, but economically advantageous. This presentation will illustrate how the principles of green chemistry can be incorporated into the innovative process across the spectrum of research, development and manufacturing worlds. Examples that demonstrate the benefits of interdisciplinary collaborations in pursuit of sustainable materials will be presented.
12:45 Lunch on Your Own (Technology Workshop, Sponsorship Available)
1:55 Chairperson's Remarks
2:00 Efficient, Environmentally Responsible
Synthesis of Aprepitant, a Potent and Orally Active NK-1 Receptor Antagonist
Dr. James McNamara, Senior Scientific Director, Process Research, Merck & Co., Inc.
A second generation process to prepare aprepitant will be described, which cuts the number of required steps in the process by one half and doubles the overall yield. This process dramatically improves the environmental impact of the production of aprepitant. A chiral secondary alcohol serves as the key raw material in the process, which in turn controls the two other asymmetric centers in the target molecule via novel and very efficient chemistry.
2:30 Green Chemistry's Role in EPA's Sustainability Agenda
Dr. Subhas K. Sikdar, Acting Associate Director for Health, National Risk Management Research Lab/ U.S. Environmental Protection Agency
United States Environmental Protection Agency has adopted the slogan, "people, planet, prosperity,” to champion the cause of sustainability. The grants program for the academia, the Presidential Green Chemistry Challenge Award, the annual Green Chemistry Conference in Washington, D.C., and laboratory-based research are the principal components through which the EPA tries to encourage the development of green synthesis methods, tools for determining environmental impact, and design methods for cleaner processes. Elimination of toxic substances, finding benign substitutes, and finding less costly ways of achieving the goals of green chemistry are the focus areas of the EPA's research in green chemistry.
3:00 "Greener" Chemical Syntheses Using Microwaves under Solvent-Free Conditions or Aqueous Media
Dr. Rajender S. Varma, National Risk Management Research Laboratory, U. S. Environmental Protection Agency
A solvent-free approach that involves microwave (MW) exposure of neat reactants (undiluted) catalyzed by the surfaces of recyclable mineral supports such as alumina, silica, clay, or 'doped' surfaces is presented which is applicable to a wide range of cleavage, condensation, cyclization, rearrangement, oxidation and reduction reactions including rapid one-pot assembly of heterocyclic compounds from in situ generated reactive intermediates. A novel aqueous N-alkylation of amines by alkyl halides that proceeds expeditiously in the presence of NaOH to deliver tertiary amines will be presented; the ensuing N-aryl azacycloalkanes are synthesized via a simple, efficient and eco-friendly protocol that involves double N-alkylation of amines. This green chemical reaction proceeds in the presence of aqueous potassium carbonate and the approach can be extended to hydrazine precursors to generate a variety of heterocyclic systems.
| 3:30 Refreshment Break, Poster and Exhibit Viewing |
Sponsored
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3:30 Refreshment Break, Poster and Exhibit Viewing
4:15 Green Chemistry - The New Paradigm for Efficiency in Pharmaceutical Development
Deborah Ross, Professional Development Program, Global Pharmaceutical Operations, Abbott Laboratories
Green Chemistry, often treated as strictly an environmental initiative, encompasses a great deal more. "Green Chemistry" is more accurately described in terms of improved design of synthetic processes, the use of emerging technologies to increase throughput, reduce waste and increase the profitability of a process. Green Chemistry is an overarching theory in efficiency which marries process chemistry and engineering to enable a life cycle approach to design and synthesis. In this talk, the basic tenets and principles of "Green Chemistry" and "Green Engineering" will be presented alongside real life examples and perspectives.
4:45 Green Chemistry is Good Process Chemistry and More
Dr. Berkeley W. Cue, Jr., Consultant, (Former VP Pharmaceutical Science, Pfizer Global R&D)
5:15 Q&A
5:30 Networking Reception in the Exhibit Hall
EXHIBIT AND SPONSOR INFORMATION
Showcase your company’s expertise, brand your solutions and develop revenue opportunities with qualified decision-makers by becoming an
Exhibitor or Sponsor of Process R&D Summit! Contract exhibit booth space by September 2, 2005 and you will save $300! If you want to discuss sponsoring
or exhibiting at Process R&D Summit, please contact Carol Dinerstein at 781-972-5471 or
dinerstein@healthtech.com
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