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QOMSBOC 2023
Plenary Speakers

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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.

Abstract:

Taming the unnatural – advancing peptide drug discovery

through diverse chemistry and collaborations

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.

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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).

Abstract:

Inventing Reactions - Catalytic activation of C-C, C-O, C-N, and C-H bonds

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.

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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.

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Bio:

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Abstract:

From Drugs to Catalysts:

Design and Application of Boron Heterocycles Guided by Properties and Reactivity

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Dennis Hall

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Christina White

Professor

University of Illinois Urbana-Champaign

Christina White was born in Athens, Greece where she grew up until the age of five. She earned her undergraduate degree in biochemistry at Smith College, where she did her thesis work with Prof. Stuart Rosenfeld in the area of host-guest chemistry. After a brief period in the biology graduate program at Johns Hopkins University, she began her doctoral studies in chemistry in Prof. Gary Posner’s lab. While in this group she initiated the hybrid Vitamin D3 analog program in his group. After completion of her Ph.D. she joined Prof. Eric Jacobsen’s lab at Harvard University as a NIH Postdoctoral Fellow where she developed the first synthetically useful methane monooxygenase (MMO) mimic system for catalytic epoxidations with hydrogen peroxide. She began her independent academic career at Harvard University and then moved to the Department of Chemistry at the University of Illinois Urbana-Champaign, where she is currently a Professor of Chemistry. White’s research lab focuses on the development of highly selective C-H functionalization methods for streamlining the process of complex molecule synthesis.

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