Last year the ACS GCI Pharmaceutical Roundtable sent a call for proposals, seeking to fund projects that are developing alternatives for widely employed transition metal catalyzed cross-coupling reactions (the assembly of carbon-carbon and carbon-heteroatom). These reactions are used frequently in the pharmaceutical industry because they allow for the assembly of compounds with significant molecular complexity (like those found in medicines). They currently depend heavily on palladium and other 2nd/3rd row transition metals that have drawbacks such as high cost, fluctuating global supply, human toxicity concerns, and limited natural abundance.
Rather than perpetuate these typical protocols the Roundtable envisions a more desirable future state for cross-coupling that not only employs non-precious/non-toxic metal catalysts, but also reduces the number of steps, achieves ambient temperature conditions, utilizes environmentally responsible solvents systems, and more. Pursuing these goals will shrink the environmental impact of medicine production, address safety conditions for workers, and reduce costs for the industry (no longer relying on rapidly depleting precious metals).
Many proposals were submitted for this call for non-precious metal catalysis, but after difficult decisions two stood out among all others.
- Dr. Paul J. Chirik received $100K for his proposal “Modern Alchemy: New Paradigms for Enabling Base Metal-Catalyzed Cross Coupling in the Pharmaceutical Industry.” Over a 2 year period, his group will at first explore the application of redox active ligands that can undergo traditional cross-coupling transformations (carbon-carbon) with a 1st row transition metal catalyst. Eventually, the team will address more long-standing challenges such as iron-catalyzed carbon-nitrogen bond formation and more.
- Dr. Daniel J. Weix of the University of Rochester received $50K for his proposal “Direct Synthesis of Alkylated Arenes and Heteroarenes from the Cross-Coupling of Heteroaromatic Halides in Non-Amide Solvents.” For the next year, Weix and his team will develop new nickel catalysts and conditions for the formation of new carbon-carbon bonds via cross-coupling. The team hopes to achieve these reactions with simple ligands and metal salts, provide broad function-group compatibility, and employ greener solvents.
Congratulations to the grant winners! Keep an eye out for updates over the coming years to see how this important research progresses. And to learn more about precious metal use in chemistry and alternative technologies, be sure to catch the Green Chemistry & Engineering Hybrid Session on June 19th, where Dr. Chirik and other experts will be presenting. Attend in person or watch the live broadcast.
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