Universities can be a major resource for industrial innovation, especially when the two collaborate to generate new knowledge and impact. Engaging with academia is key to the strategy of the ACS Green Chemistry Institute’s Pharmaceutical Roundtable. Year after year, the Roundtable delivers on this priority by providing grants for academic-industrial research collaborations ($1.5 million since 2005) and hosting events that act as a bridge between university research and company application. To kick off their 10-year anniversary celebrations, the Roundtable hosted an all-day catalysis symposium in conjunction with their Spring Meeting in Basel, Switzerland.
Roland Thieme, the Head of Chemical Development and Supply at F. Hoffmann-La Roche (the co-host of the symposium), and Juan Colberg, Senior Director at Pfizer and co-chair of the Roundtable, opened the symposium. Their introduction illustrated how the title of the event, “Green Chemistry Makes a Difference: Innovations leading to a more sustainable pharmaceutical industry,” summarizes the mission of the Roundtable—to catalyze the implementation of green chemistry and engineering in the global pharmaceutical industry. For 10 years, the Roundtable has executed on this mission based on their strategic priorities (to inform and influence the research agenda, provide tools for innovation, act as an education resource, and collaborate globally) and, since 2007, a set of key research areas. These research areas are topics that all companies were consistently encountering and seeking greener alternatives for. They were determined via a brainstorming and voting process by the Roundtable, which resulted in three categories the group would target for the next eight years in their initiatives: reactions currently used but better reagents preferred, more aspirational reactions, and solvent themes.
A theme that persists throughout most of these key research areas is catalysis, a fundamental pillar of green chemistry. The Roundtable seeks to not only further employ catalyst technologies in pharmaceutical science, but ensure that the approaches are greener than what currently exist (such as moving away from use of precious metal catalysts). With the goal of triggering innovation in approaches to and applications of catalysis technologies, the symposium in Basel featured six professors based in Europe who are leaders in the field and hosted nearly 20 posters from students, academics, and industry professionals.
Symposium speakers from left to right: Marc Taillefer, Uwe Bronscheuer, Katalin Barta, Benjamin List, Janine Cossy, and Michael North.
“The Roundtable convenes events like this symposium to foster discussion between academic and private sector around potential greener commercial approaches, by influencing the new technology research agendas. We are very excited to host these distinguished speakers, as each address important and innovative approaches to make organo, enzymatic, and transition metal catalysis in pharmaceutical science more sustainable. These professors are discussing some of the biggest problems facing the industry with respect to catalysis such as limited supply, toxicity, cost, and solvent volume. One example is the strides made around minimizing the use of precious metals by looking to more sustainable options like iron, nickel and copper--metals that are obtained via cleaner mining processes and provide lower supply risk from more stable mining conditions. Additionally, catalytic methods to access renewable raw materials from biomass were highlighted, establishing sustainable alternatives to petroleum products needed to make life-saving medicines” said the Roundtable co-chairs.
The first talk was from Professor Benjamin List of the Max Planck Institute—Mülheim (Germany), who discussed an approach to enantioselective synthesis called “asymmetric counteranion directed catalysis.” This technique can be applied to several reactions (such as alylation, phosphylation, etc.), many of which are frequently employed by the pharmaceutical industry. List was followed by Professor Katalin Barta of University of Gronigen (Netherlands). She focused on strategies for the conversion of biorenewables through sustainable catalysis with earth abundant metals. The approaches Barta presented not only provide catalytic innovations for the industry, but will lead to renewable-based (rather than petroleum) starting materials the industry depends on everyday as reagents and solvents. Professor Marc Taillefer of ENSC Montpellier (France) wrapped up the first half of talks with his work, which utilizes copper and iron catalysts that allow for a wide range of transformations (achieving C-C, C-O, and C-N bonds) under significantly milder conditions than traditional approaches.
Between the talks and during meals throughout the day, attendees were able to peruse the poster session highlighting work ranging from one-pot cascade reactions to ball-milling as a solventless reaction. “I genuinely believe that society cannot continue at current consumption levels, and as chemists we can address this by moving towards new, sustainable approaches, such as batch to flow processes. This symposium has brought together a lot of people from many companies, yet is small enough so that everyone can talk to everyone and discuss real-world problems and solutions,“ said G. Kemeling, the Editor in Chief of ChemSusChem.
After lunch, the symposium attendees flowed back into the auditorium to hear Professor Uwe Bornscheur of University of Greifswald (Germany) discuss enzyme discovery, engineering, and application in biocatalysis. Bornscheur walked the audience through the history of how enzymatic processes have been able to replace chemical routes, and used his work to show a broad range of enzyme-catalyzed reactions that are efficient, highly selective, and can be achieved under mild conditions with less by-products than equivalent chemical routes. Professor Janine Cossy of ESPCI Paris (France) followed with a talk filled with approaches to cyclization and coupling that replace palladium catalysts with a variety of alternative and greener catalysts (such as the more abundant iron). The molecules she focuses on (macrocyclic) are currently under-exploited by industry (accounting for only 2% of orally available molecules on the market, currently useful for anti-tumoral activity), but her work can deliver steps to these molecules with more benign chemistry. The symposium closed with Professor Micheal North from University of York and the Green Chemistry Centre for Excellence (England). His talk highlighted his group's bimetallic catalytic approach that allows for transformation of carbon dioxide to cyclic carbonates, as well as applications of these carbonates as green solvents. By making use of waste CO2 and moving towards flow chemistry, the research is delivering ethylene carbonate and propylene carbonate as possible solvent replacements for DMF, DMSO, and other toxic media sometimes present in pharmaceutical science. Another emphasis of North's talk was the importance of outreach, to both student groups and industry, which the Centre incorporates into each of their project areas.
John Tucker, a senior scientist at Amgen and co-chair of the Roundtable, closed the day's events with a summary of how these talks had already instigated much inspiration and conversation for future innovation. Whether it was the elegant cascade reactions facilitated by enzymes or the replacement of unsustainable metal catalysts, the symposium offered a wide array of technologies that have the potential to transform the industry. As the Roundtable looks to their next ten years they aspire to continue delivering on their strategic priorities, and bridge academic and industrial communities throughout the world to make their science more sustainable. The 10-year anniversary celebrations will continue throughout the year, with the next events taking place at the 19th Annual Green Chemistry and Engineering Conference in the Washington, DC area (USA) and the 250th ACS National Meeting and Exposition in Boston, MA (USA). The Roundtable will also be releasing an update of their key research areas, discussing new focus areas, as well as actions and progress to date. For more information, please visit the Pharmaceutical Roundtable’s website and for Roundtable updates and announcements, follow ACS GCI on social media (Twitter, Facebook, and LinkedIn).
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