RT 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. The Medicinal Chemistry sub-Team is organized for best practice sharing and have identified a variety of useful practices to green medicinal chemistry.
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. J. Med. Chem., 2013, 56 (15), pp 6007–6021.
Sustainable Practices in Medicinal Chemistry Part 2: Green by Design
Aliagas, Ignacio; Berger, Raphaëlle; Goldberg, Kristin; Nishimura, Rachel T.; Reilly, John; Richardson, Paul; Richter, Daniel; Sherer, Edward C.; Sparling, Brian A.; Bryan, Marian C. J. Med. Chem. 2017, 60 (14), pp 5955–5968.
Improve the sustainability of the pharmaceutical industry in early discovery projects.
2019 RFP for precious-metal free cross-coupling methodology for med. chem.
2018 Photochem grant with Prof. Stephenson is completed. Scott Plummer, Novartis, is the Roundtable lead. “Microfluidic reactor and late-stage functionalization of diverse scaffolds”
Updated: March 2021
- First Precious metal-free cross-coupling RFP meeting
- Follow up RFP (Prof. Yoon). Points-of-contact (primary: Charles Yeung; secondary: Paul Richardson), both using feedback from across entire team
- Seek for funding opportunities in future RFP
- The team is focused on writing a manuscript ranking replacements for unsustainable solvents on reactions and work ups.
- The analysis of unsustainable solvent usage in early development by reaction class is ongoing.
- Offer greener alternatives to those reaction classes typically run in unsustainable solvents.
- Brainstorming a way to rank and prioritize solvent selection for work ups.
- Influence vendors to provide competitive prices of green neoteric solvents.
- Yoon RFP: meeting follow up (Q4 2021)
- Manuscript submission (Q4 2021)
The Team has been holding outreach workshops and seminars at universities including UCSD, UMass Boston, MIT and Stanford in 2018.