The ACS GCI Pharmaceutical Roundtable has identified key synthetic chemistry and process research challenges whose solutions would result in more efficient pharmaceutical process development and production. To spur research in these areas, the Roundtable created and maintains a research grant program, whose impact over the years has been recently documented. The Roundtable also advocates for targeted green chemistry and engineering support to academic and government labs from international and U.S. federal funding agencies.
Key Research Areas
In 2007, the Roundtable published a seminal paper outlining the most relevant and promising green chemistry research areas within the pharmaceutical industry. The paper provides industry insight for academic researchers interested in pharmaceutical research and has been widely cited.
The Roundtable published an update to this paper in 2018:
Key Green Chemistry research areas from a pharmaceutical manufacturers’ perspective revisited. Marian C. Bryan, Peter J. Dunn, David Entwistle, Fabrice Gallou, Stefan G. Koenig, John D. Hayler, Matthew R. Hickey, Shaun Hughes, Michael E. Kopach, Gerard Moine, Paul Richardson, Frank Roschangar, Alan Steven and Franz J. Weiberth. Green Chem., 2018, 20, 5082.
12 Key Research Areas
- Development of effective and versatile methodology utilizing cheap/sustainable metals.
- General methods for catalytic/sustainable (direct) amide or peptide formation.
- Aliphatic and aromatic C–H activation, using green oxidants and giving predictable site selectivities.
- Amide reductions avoiding LiAlH4 and diborane.
- Direct substitution of alcohols.
- Catalyst immobilization without significant loss in kinetics.
- Asymmetric hydrogenation of unfunctionalized olefins/ enamines/imines.
- Improved fluorination/trifluoromethoxylation.
- Wittig chemistry without Ph3PO.
- Alternatives for oxidations, C–O or C–N redox processes.
- Viable replacements for polar aprotic solvents.
- Viable replacements for halogenated solvents.
Over $2 million dollars (US) have been funded by the ACS GCI Pharmaceutical Roundtable since their grant program began in 2007. Each Spring, new Request for Proposals (RFPs) are issued for different key research challenges faced by the Pharmaceutical industry.
2019 ACS GCI Pharmaceutical Roundtable Research GrantProposal to Determine the Potential Scope and Environmental Impact of Analytical and Preparative-Scale Supercritical Fluid Chromatography Processes
ACS GCIPR is seeking to fund a 12-month R&D collaboration to support the goal of the Roundtable’s analytical chemistry initiative to clearly define sustainable chromatographic analytical and purification methodologies applied across the pharmaceutical industry. Proposals are invited from public and private institutions of higher education worldwide. One grant will be awarded. The proposal deadline is July 1, 2019 by 5 p.m. EDT (GMT-4).
2019 ACS GCI Pharmaceutical Roundtable Research Grant for Greener Medicinal Chemistry
ACS GCIPR is seeking to fund a 12-month R&D commitment to assist the Roundtable’s medicinal chemistry initiative. The focus of the R&D will be toward the development of precious metal-free cross-coupling methodology applicable to substrates such as heterocycles that are widely used in the industry. Proposals are invited from public and private institutions of higher education worldwide. One grant will be awarded, and the total award is limited to $50,000. The proposal deadline is July 1, 2019 by 5 p.m. EDT (GMT-4).
2019 ACS GCI Pharmaceutical Roundtable Ignition Grant Program for Green Chemistry and Engineering Research
ACS GCIPR is seeking to provide ‘ignition’ funding for novel and innovative ideas that have the potential to provide sustainable solutions to chemistry and engineering problems relevant to the pharmaceutical industry from discovery to manufacturing. The goal is to provide researchers with initial funding to obtain preliminary results that may then be used by the researchers to help apply for funding from traditional funding agencies. Proposals are invited from public and private institutions of higher education worldwide. Up to four grants of $25,000 will be awarded. The proposal deadline is July 1, 2019 by 5 p.m. EDT (GMT-4).
See previously awarded ACS GCI Pharmaceutical Roundtable grants
Song Lin, Cornell University, $25,000
“Electrocatalytic Fluorination Reactions Using Sustainable Fluorine Sources”
Benjamin Wiley, Duke University, $25,000
“C-H/C-H Cross-Coupling of Aromatic Compounds with Flow-Through Nanowire Electrode”
Jennifer L. Stockdill, Wayne State University, $50,000
“Catalytic Desulfurization of Peptides”
Corey Stephenson, University of Michigan, $50,000
“A Microfluidic Platform for Discovery and Optimization of Photoredox Reactions”
Jennifer L. Stockdill, Wayne State University, $50,000
“A Green Strategy for the Synthesis of Head-to-Tail Macrocyclic Peptides”
James Kiddle, Western Michigan University, $25,000
“The Wittig Reaction Metamorphosis from Phosphorus to Boron”
Stephen G. Newman, University of Ottawa, $25,000
“Using Flow Chemistry to Harness Ozone as a Sustainable Oxidant for C–H Functionalization”
Andrew Texeira, Worcester Polytechnic Institute, $25,000
“Enhanced Site-Accessibility for Solid-Phase Coupling in Hierarchical Materials”
Dennis Hall, University of Alberta, $25,000
“Borate-Based Catalytic Directing Groups for Alkene and C–H Functionalization Reactions Using Readily Available Alcohol Substrates”
Oana Luca, University of Colorado – Boulder, $25,000
“Catalyst and Electrolyte-Free Direct Electrochemical Cross Coupling”
Jeff Byers, Boston College, $25,000
“Development of an Iron-Based Catalyst for Suzuki-Miyaura Cross Coupling Reactions”
Zach Amara, National Des Arvts Et Métiers, $25,000
“Smart Synthesis with Magnetically Recoverable Visible Light Photocatalysts”
Leo Choe Peng, Universiti Sains Malaysia, $16,000
“Diafiltration of Monoclonal Antibody using pH Responsive Membrane with Positive Charge.
Andrew Zydney, Penn State, $50,000
“Countercurrent Staged Diafiltration for Monoclonal Antibody Formulation.”
Amanda Evans, California State University, Fullerton, $50,000
“Enz-Flow/Continuous Bioprocessing: Towards a green continuous flow synthesis of levomilnacipran”
A. John Blacker, University of Leeds, $50,000
“Process Development of Continuous Flow Oxidative Biotransformations.”
Graham Dobereiner, Temple University, $50,000
“Tandem Catalytic Process in Flow: Synthesis of amides via mild photochemical carbonylation using CO2 as a carbonyl source.”
Amanda C. Evans, California State University, $50,000
“Enz-Flow/Continuous Bioprocessing: Towards a green continuous flow synthesis of levomilnacipran.”
Matthias Beller, Leibniz-Institut für Katalyse, $50,000
“Hydrogenation of Amides promoted by Ru- and Fe-Pincer Complexes—Ligand-Metal Cooperative Catalysis for the Mild and Selective Synthesis of Amines”
Neal Mankad, University of Illinois at Chicago, $100,000
“Bimetallic Approach to Iron-Catalyzed Coupling Reactions”
Paul Chirik, Princeton University, $100,000
“Modern Alchemy: New Paradigms for Enabling Base Metal-Catalyzed Cross-Coupling in the Pharmaceutical Industry”
Daniel Weix, University of Rochester, $50,000
“Direct Synthesis of Alkylated Arenes and Heteroarenes from the Cross-Coupling of Heteroaromatic Halides in Non-Amide Solvents”
Janet Scott, University of Bath, $100,000
“Intelligent Selection of Greener Solvents”
Neil Garg, UCLA, $60,000
“Development of Green Nickel-Catalyzed Cross-Coupling Reactions”
Shannon Stahl, University of Wisconsin-Madison, $150,000
“Oxidation/Epoxidation Methods Without the Use of Chlorinated Solvents: Chemoselective Aerobic Alcohol Oxidation Catalyzed by Earth-Abundant Metals”
Wei Zhang, University of Massachusetts-Boston, $25,000
“Greener Grignard Reactions”
Charles Liotta, Georgia Tech University, $150,000
“Green and Effective Continuous Catalytic Homo-Nazarov Cyclization Towards Multi-Step Synthesis of Heteroaromatic Ring-Fused Clyclohexanones”
David Cole-Hamilton, University of St. Andrews, $150,000
“Amide Hydrogenation to Amines”
Robert Crabtree, Yale University, $160,000
“Atom Economic Alcohol Activation and Amide Synthesis Using Base-Metal Catalysts Heterogenized on Titania Nanoparticles”
Chao-Jun Li, McGill University, $130,000
“Chiral Amines via Asymmetric Multi-component Reactions”
Michael Krische, University of Texas-Austin, $129,000
“Byproduct-Free Synthesis of Chiral Amines via C-C Bond Forming Transfer Hydrogenation and Hydrogen Auto-Transfer”
Robert Maleczka and Milton Smith, Michigan State University, $100,000
“Catalytic C-H Activation/Cross-Coupling of Aromatics (Avoiding the Preparation of Haloaromatics)”
Jianliang Xiao, University of Liverpool, $126,166
“Hydrogenation of Amides by Multifunctional Catalysts via Ground State Destabilisation”
Impact of Grant Program
To date, 28 research programs have been funded globally on topics such as C–H activation, flow chemistry, biocatalysis, novel catalytic transformations, base metal catalysis, and solvent substitution. From these research projects, 73 peer-reviewed publications have resulted with over 1700 unique daughter citations (see reference below).
Evaluating the Impact of a Decade of Funding from the Green Chemistry Institute Pharmaceutical Roundtable
Stefan G. Koenig, David K. Leahy, and Andrew S. Wells
Org. Process Res. Dev., 2018, 22 (10), 1344-1359.
In addition to the publications resulting from the grant program, the Roundtable is a frequent and influential publisher on a variety of topics. Recent publications include:
- Evaluating the Impact of a Decade of Funding from the Green Chemistry Institute Pharmaceutical Roundtable, Stefan G. Koenig, David K. Leahy, and Andrew S. Wells, Org. Process Res. & Dev. 2018, 22 (10), 1344-1359. DOI: 10.1021/acs.oprd.8b00237
- Green Chemistry Articles of Interest to the Pharmaceutical Industry; Org. Process Res. Dev. 2018, 22, (6), 667-680, DOI: 10.1021/acs.oprd.8b00056
- Inspiring Process Innovation via an Improved Green Manufacturing Metric: iGAL, Green Chem., 2018, 20, 2206-2211. DOI: 10.1039/C8GC00616D