QOMSBOC 2023
Plenary Speakers
Dani Schultz, Ph.D.
Director, Discovery Process Chemistry
Department of Process R&D
Merck, Kenilworth, NJ
USA
Bio:
Dani Schultz received her PhD from the University of Michigan working with Professor John Wolfe and was an NIH postdoctoral fellow at the University of Wisconsin-Madison with Professor Tehshik Yoon. Since joining Merck in 2014, Dani has been a member of Process Chemistry and Enabling Technologies in Rahway, NJ and as of 2021 became the Director of the Discovery Process Chemistry group in Kenilworth, NJ where she leads a group of process chemists in support of the Merck small molecule and peptide portfolio. Throughout her time at Merck, Dani has been involved in the development of synthetic routes for drug candidates spanning HIV and oncology – forging meaningful collaborations, both internally and externally, to address the synthetic challenges that occur during pharmaceutical development.
Dani is an advocate for DEI in STEM by organizing and hosting several internal events around diversifying chemistry and most recently, she has served as co-host to the Pharm to Table Podcast (@PharmToTablePodcast) that aims to elevate the people and stories behind #MerckChemistry.
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Abstract:
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Taming the unnatural – advancing peptide drug discovery
through diverse chemistry and collaborations
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Non-naturally occurring peptides are a growing therapeutic modality with most applications targeting endogenous proteins; however, advances in hit-to-lead platforms (such as mRNA display and DEL) have revealed that the druggable space of peptides can be greatly expanded. As a result, the discovery of peptide therapeutics is rapidly evolving and there is a growing need to dive into the non-canonical amino acid pool in order to fine tune biopharmaceutical properties such as potency, bioavailability and cell permeability. Through internal partnerships and academic-industrial collaborations, we have developed several methods to access non-canonical amino acids impacting both naturally occurring and synthetic peptides. A common thread throughout this work will be how sharing industrial challenges with our academic collaborators, coupled with our internal capabilities, can quickly transform ideas into impactful solutions.
Lukas Gooßen, Ph.D.
Professor, Evonik Chair
of Organic Chemistry
Ruhr-Universität Bochum
Germany
Bio:
Lukas Gooßen studied Chemistry at the universities of Bielefeld and Michigan and performed his master thesis in the group of K. P.C. Vollhardt at UC Berkeley. He was awarded a Ph.D. in 1997 for research on N-heterocyclic carbene complexes supervised by W.A. Herrmann at the TU Munich, and pursued postdoctoral research with Nobel laureate K.B. Sharpless. He began his professional career as an industrial chemist at Bayer AG in 1999, then moved back to academia to the group of M.T. Reetz, MPI for Coal Research for his Habilitation, and further to RWTH Aachen. From 2005-2016 he was professor at the TU Kaiserslautern, in 2008, he was visiting professor at the University of Toronto. In 2016, Lukas Gooßen was appointed Chair of Organic Chemistry at the RU Bochum.
His research is devoted to the development of novel concepts for C-C- and C-heteroatom bond formation designed to reduce the production of waste salts and effluents. He received the Jochen-Block award of the DECHEMA (2003), the Carl-Duisberg Award of the GDCh (2007), the Novartis Young Investigator Award (2007), and the AstraZeneca Award in Organic Chemistry (2008).
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Abstract:
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Inventing Reactions - Catalytic activation of C-C, C-O, C-N, and C-H bonds
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Over the past decade, decarboxylative coupling reactions, i.e. reactions in which C–C bonds to carboxylate groups are cleaved with formation of new carbon–carbon bonds, have evolved into a powerful synthetic strategy.1 Their key benefit is that they draw on easily available carboxylic acids rather than expensive organometallic reagents as sources of carbon nucleophiles. Decarboxylative couplings have been utilized in syntheses of biaryls, vinyl arenes, fluoroalkyl compounds and aryl ketones. Decarboxylative Chan-Evans-Lam alkoxylations and aminations of benzoic acids as well as electrodecarboxylative C-O bond forming reactions demonstrates that this reaction concept is applicable also to C–heteroatom bond-forming reactions. Carboxyl groups can also function as deciduous directing groups that stay in place just long enough to guide a C-H functionalization step into a specific position and are shed tracelessly as soon as it is accomplished.
In this presentation, the rational, yet creative process of catalytic method development will be illustrated for these and other sustainable C–C and C–heteratom bond-forming reaction such as salt-free C-H carboxylations,2 C-H allylations,3 or para-selective C-H arylations.4
References:
1) (a) L. J. Gooßen, G. Deng, L. M. Levy, Science 2006, 313, 662–664. (b) M. Pichette Drapeau, J. Bahri, D. Lichte, L. J. Gooßen, Angew. Chem. 2019, 58, 892–896. (c) G. Zhang, Z. Hu, F. Belitz, Y. Ou, N. Pirkl, L. J. Gooßen, Angew. Chem. 2019, 131, 6501-6505 (d) Á. M. Martínez, D. Hayrapetyan, T. van Lingen, M. Dyga, L. J. Gooßen, Nat. Commun. 2020, 11, 4407.
2) T. van Lingen, V. Bragoni, M. Dyga, B. Exner, D. Schick, C. Held, G. Sadowski, L. J. Gooßen, Angew. Chem. Int. Ed. 2023, e202303882.
3) (a) J. F. Goebel, J. Stemmer, F. Belitz, L. J. Gooßen, Angew. Chem. Int. Ed. 2023, e202301839; (b) A. S. Trita, A. Biafora, M. Pichette-Drapeau, P. Weber, L. J. Gooßen, Angew. Chem. Int. Ed. 2018, 57, 14580-14584.
4) D. Lichte, N. Pirkl, G. Heinrich, S. Dutta, J. F. Goebel, D. Koley, L. J. Gooßen, Angew. Chem. Int. Ed. 2022, e202210009.
Dennis Hall
Professor
University of Alberta
Edmonton, Canada
Bio:
Dennis Hall received his PhD in 1995 working with Prof. Pierre Deslongchamps at the Université de Sherbrooke (Quebec, Canada). Between 1995–1997 he was an NSERC PDF in the group of Prof. Peter G. Schultz at UC Berkeley. He moved to the University of Alberta in 1997 where he currently holds the Tier-1 Canada Research Chair in Boron Chemistry for Catalysis and Drug Discovery. The unifying theme of his interdisciplinary research program is the development of new synthetic and biological applications of organoboron derivatives, including catalysis, stereocontrolled reactions, heterocyclic chemistry, and medicinal chemistry. He has co-authored over 170 peer-reviewed publications with his group members and his contributions were recognized by a number of awards, including a national Killam Research Fellowship (2019–2021), the 2021 R. U. Lemieux Award from the Canadian Society for Chemistry, and a 2024 Arthur C. Cope Scholar Award from the American Chemical Society. In 2017, he was Elected a Fellow of the Royal Society of Canada (FRSC). He currently serves as an Associate-Editor of Science Advances (AAAS), and he is a member of the Editorial Board of Organic Reactions (Wiley).
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Abstract:
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From Drugs to Catalysts:
Design and Application of Boron Heterocycles Acids Guided by Properties and Reactivity
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The commercialization of benzoxaborole drugs has sparked a renaissance surrounding heterocycles derived from boronic acids in organic and medicinal chemistry, where they demonstrate a wide range of biological properties. Despite this success, many questions remain unanswered regarding the physical properties, acidic nature (Lewis vs Brønsted), dynamic behavior, and reactivity of boranol (B–OH)-containing heterocycles in organic and aqueous media. To resolve decades of conflicting views on the acidic and aromatic characteristics of pseudoaromatic hemiboronic acids, our laboratory reported multipronged experimental and computational approaches. These fundamental studies are essential for guiding a systematic application of select boroheterocycles as enantioselective reaction catalysts, in bioconjugation, and as new antibacterial drug chemotypes and bioisosteres of pharmaceutically important classes of heterocycles. In recent work, benzoxazaborine derivatives were identified as modular scaffolds enabling both nucleophilic and electrophilic catalytic activation of alcohols. Ongoing work investigates the exchangeability of B–OH bonds for direct catalytic activation of alcohols and diols under thermal and photochemical conditions.
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