Medicinal Chemistry
Roundtable member companies invest heavily in the discovery of new active pharmaceutical ingredients. Key to the success of these efforts are synthetic organic chemists who rapidly develop large libraries of synthetic analogues that are screened for potential activity against a particular disease target. There is an emphasis on the rapid identification of synthetic routes that lead to the isolation of sufficient active ingredient to perform early discovery studies. This emphasis on speed usually results in highly inefficient reaction schemes, isolations and work-ups. By sharing best practices, Roundtable member companies have identified a variety of useful practices to green medicinal chemistry.
Related Resources
Practical Considerations for a More Sustainable Medicinal Chemistry DMTA Lifecycle
Covering topics such as in silico tools to filter compound designs to reduce the number of compounds being synthesized; direct to biology type technologies; practical methods to carry out ‘greener chemistry’ for example novel (more efficient/sustainable) methodologies for classical reaction types; new purification methods; alternative reagents to avoid toxic/environmentally damaging reagents; reaction miniaturization efforts for Medicinal Chemistry (beyond hit finding).
Session Organizers: Paul Richardson, Pfizer; Kristy Anderson, Boehringer Ingelheim; Alvaro Enriquez Garcia, Lilly.
GC&E Conference
Presented at the
This session will be presented at the 29th Annual Green Chemistry & Engineering Conference, which will be held in Pittsburgh, PA, on June 23-26, 2025. Call for abstracts is open January 3–February 14, 2025. For more information, see www.gcande.org.
Selective reduction of aromatic rings in advanced scaffolds in flow reactors with non-noble metal catalysis under mild conditions
Jack Norton and Aaron Moment, Columbia University, $50,000 “Selective reduction of aromatic rings in advanced scaffolds in flow reactors with non-noble metal catalysis under mild conditions”
Tunable Catalytic C(sp3)-H Functionalization of Heterocyclic Scaffolds
Jennifer Schomaker, University of Wisconsin-Madison, $50,000 “Tunable Catalytic C(sp3)-H Functionalization of Heterocyclic Scaffolds”
C–N Attached-Ring Synthesis by Markovnikov Hydroamination
Ryan Shenvi, Scripps Research, $50,000
“C–N Attached-Ring Synthesis by Markovnikov Hydroamination”
A Microfluidic Platform for Discovery and Optimization of Photoredox Reactions
Corey Stephenson, University of Michigan, $50,000
“A Microfluidic Platform for Discovery and Optimization of Photoredox Reactions”
Sustainable Practices in Medicinal Chemistry Part 2: Green by Design
Sustainable Practices in Medicinal Chemistry Part 2: Green by Design J. Med. Chem. 2017, 60, 5955-5968. DOI: 10.1021/acs.jmedchem.6b01837
Sustainable Chromatography (an oxymoron?)
Sustainable Chromatography (an oxymoron?) Emily A. Peterson, Barry Dillon, Izzat T. Raheem, Paul Richardson, Daniel Richter, Rachel Schmidt, and Helen F. Sneddon. Green Chem. July 14, 2014 (web), DOI: 10.1039/C4GC00615A
Sustainable Practices in Medicinal Chemistry: Current State and Future Directions
Sustainable Practices in Medicinal Chemistry: Current State and Future Directions Bryan, Marian C.; Dillon, Barry; Hamann, Lawrence G.; Hughes, Gregory J.; Kopach, Michael E.; Peterson, Emily A.; Pourashraf, Meharnez; Raheem, Izzat; Richardson, Paul; Richter, Daniel; Sneddon, Helen. J. Med. Chem. [online early access] DOI:10.1021/jm400250p. Published Online: April 15, 2013.