SYNTHETIC DESIGN IN GREEN CHEMISTRY

Greener Approaches to Therapeutic Synthetic Polypeptides– Oral
Tuesday PM

Symposium Organizer: Kristi Budzinski (Genentech); ACS GCI Pharmaceutical Roundtable

Biologics are a widely diverse group of therapeutic compounds including peptides, antibodies, non-antibody proteins, and vaccines and are a growing sector of the pharmaceutical market.  Typically manufactured by living cells, biologics generate less chemical waste than small molecule pharmaceuticals but consume large quantities of water and energy and significant volumes of single-use plastics and filters. Several initial environmental analyses have been performed for biologics production and underscore the need for incorporating sustainability into the development process. As a half-day symposium, this session aims to highlight currents efforts in biologics process research and development and manufacturing to incorporate green chemistry and engineering principles. Specifically it will highlight innovative engineering processes and technologies that can reduce energy and water usage and waste generation and tools for measuring environmental impacts along the production chain.  Next generation therapeutics such as antibody drug conjugates (ADCs), therapeutic polypeptides, antisense oligonucleotides (ASOs), bispecific antibodies and related compounds are changing the landscape of bioprocessing and small molecule development. This session will explore how green chemistry and engineering practices can contribute to the sustainable design of bioprocess methods for next generation therapeutics.

Driving Waste Toward Zero: The Importance of Superior Process Design- Oral
Tuesday PM

Symposium Organizer: David Leahy (Bristol-Myers Squibb); ACS GCI Pharmaceutical Roundtable

Session Chair: JJ (Jingiun) Yin (Merck)

While efficient, concise and convergent synthetic routes to complex molecules are essential for their sustainable production; of equal importance is the efficiency of individual processes that comprises each step along the synthetic route.   Thus excellent process design enables sustainable chemical synthesis on industrial scale.  This session will explore how improved synthetic methodologies, catalysis, solvent selection, recycling, and minimization of unit operations play a vital role in process chemistry allowing waste generation to drive towards zero.

New Sustainable Synthetic Strategies Through Photoredox Catalysis- Oral
Wednesday AM

Symposium Organizer: David Leahy (Bristol-Myers Squibb); ACS GCI Pharmaceutical Roundtable

Session Chair: Neil Strotman (Bristol-Myers Squibb)

Visible light photoredox catalysis represents a new and exciting mode of catalytic activation of organic molecules, and has recently spurred intense interest across the organic chemistry community.  Photoredox catalysis has enabled the design of powerful new transformations through single-electron transfer (SET) pathways, using safe, bench stable catalysts.  This session will explore the design, and development of new photoredox transformations and their application to green and sustainable chemical synthesis.

Green Chemistry & Medicinal Chemistry are Miscible! -Oral
Wednesday PM

Symposium Organizer: Stefan Koenig (Genentech); ACS GCI Pharmaceutical Roundtable

Session Chair: Dan Richter (Pfizer)

Medicinal chemists are charged with the rapid synthesis of a large group of chemical structures to find hits for their biological target of interest and then optimize these hits these into lead candidates.  As a result of reliance on tried and true synthetic methods, non-green chemicals, solvents, and conditions are often part of the initial chemical synthesis of any given investigative compound.  These non-green synthetic procedures are then often adapted by process chemists to make large-scale deliveries in order to meet tight timelines.  However, through recent progress in developing greener methods to many common transformations, the process of drug discovery has become more sustainable and these initiatives can accelerate the pace of molecules in the pharma pipeline by facilitating more ready adaptation by process chemists.  By leveraging modern synthetic methods (C-H activation, aqueous chemistry, biocatalysis, etc.) and more practical considerations (electronic notebooks, smarter solvent choices, and chromatography minimization), speed to clinic can be enhanced because more sustainable chemistry is practiced.  Broadening the application of Green Chemistry into Medicinal Chemistry is at the leading edge of the ACS Green Chemistry Institute Pharmaceutical Roundtable’s mission and several breakthroughs will be featured in this symposium.

How to get there from Here: Sustainably- Oral
Wednesday AM

Symposium Organizer: Stefan Koenig (Genentech); ACS GCI Pharmaceutical Roundtable

Session Chair: Chris Beaudry (Oregon State University)

The efficient synthesis of complex pharmaceuticals and natural products is a longstanding problem facing the chemistry community.  As the industry gravitates towards more complex molecules in order to access new targets and therapies, it is vitally important that synthetic strategy keeps pace so that these new drugs are made available to patients.  This session will explore the importance of synthetic route design, not only to manufacture biologically active molecules in a sustainable fashion, but also to expand the scope of what chemical synthesis can offer on a commercial scale.

Advances in Continuous Chemistry: Back to the Future- Oral
Tuesday AM

Symposium Organizer: Michael Kopach (Eli Lilly); ACS GCI Pharmaceutical Roundtable

For many decades flow chemistry has been used extensively in the petrochemical industry for its increased safety, efficiency and product quality. Many of these benefits are also directly applicable to orthogonal industries. For these reasons continuous chemistry has recently been gaining interest in academia and the pharmaceutical industry. This session will focus on development of novel continuous chemistry designed to improve safety, quality and efficiency. Papers for this session should address:

New chemistries which are operated optimally in continuous flow mode.

Gas phase reactions in explosive regimes

Highly exothermic, high temperature or cryogenic processes

Integrated synthesis, work-up and analysis

Case studies with a focus on process safety and material efficiency.

Comparative analyses using metrics which measure sustainability. These include Process Mass Intensity (PMI) and Global Warming Potential (kg / CO2 eq.)

New Directions in Green Synthetic Design- Oral
Thursday PM