Innovation in the Synthesis of Complex Pharmaceuticals

Main list: RSC Award Lectures


Dr Martin Eastgate - RSC Organic Industrial Chemistry Award Winner
Bristol-Myers Squibb
Innovation in the Synthesis of Complex Pharmaceuticals Martin D. Eastgate
Bristol-Myers Squibb, 1 Squibb Drive, New Brunswick, NJ, 08903 USA
Email: Modern pharmaceuticals are both increasingly complex 1 and increasingly diverse. Today’s clinical candidates often contain challenging stereochemistry, unique molecular architectures, and uncommon heterocyclic frameworks; they range from small molecules to natural products, peptides, oligonucleotides, antibody-drug conjugates and other modalities. Developing safe, scalable and efficient approaches to these molecules, in the context of increasingly short development timelines, requires an approach focused on maximizing impact through innovative chemical solutions – so called ‘disruptive innovations’. 2 However, increasing complexity brings challenges in the decision making process, impacting our ability to identify which chemical strategies will optimize sustainability. These decisions can be aided by predictive decision making tools, cognizant of potential environmental impact, and recent advances have begun to establish such methodologies. 3 This presentation will cover the synthetic strategies and chemical innovations developed to address several clinical candidates from the Bristol-Myers Squibb portfolio. Our approach 2 has led to the invention of several new synthetic approaches, 4 new chemical methods, 5-8 and new concepts in predictive data analytics. 3
[1] Li, J., Eastgate, M. D.; Org. Biomol. Chem., 2015, 13, 7164. [2] Eastgate, M. D., Schmidt, M. A., Fandrick, K. R., Nature Reviews: Chemistry, 2017, 1, 16. [3] Li, J., Borovika, A., Albrecht, A., Eastgate, M. D., ACS Green Chem. & Eng., 2018, 6, 1121; Li, J. and Eastgate, M. D., RSC React. Chem. & Eng., DOI: 10.1039/c9re00019d; Borovika, A. et al., ChemRxiv DOI 10.26434/chemrxiv.7594646.v1. [4] Schmidt, M., Simmons, E. M., Wei, C. S., Li, H., Eastgate, M. D., J. Org. Chem., 2018, 83, 3928. [5] Knouse, K. W., et al, Science 2018, 361, 1234 [6] Foo, K., Sella, E., Thome, I., Eastgate, M. D., Baran, P. S., J. Am. Chem. Soc., 2014, 136, 5279. [8] Kheirabadi, M., Creech, G., Nirschel, D., Qiao, J., Leahy, D., Boy, K., Carter, P., and Eastgate, M. D., J. Org. Chem., 2018, 83, 4323.
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  • Venue

    Theatre C, Purdie

  • Date

    January 22, 2020

  • Time

    From: 14h00 To: 15h00

  • Sponsor

    Royal Society of Chemistry

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