NESACS Process Chemistry Symposium Oct. 12, 2017

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Speakers Bios for the October 12, 2017
Process Chemistry Symposium

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Stephen Buchwald - Massachusetts Institute of Technology

Stephen L. Buchwald was born (1955) in Bloomington, Indiana.  He received his Sc.B. degree from Brown University in 1977 where he worked with Kathlyn A. Parker and David E. Cane at Brown University as well as Professor Gilbert Stork at Columbia University.  He entered Harvard University as a National Science Foundation Predoctoral Fellow in 1977 and received his Ph.D. in 1982.  His thesis work, with Jeremy R. Knowles, concerned the mechanism of phosphoryl transfer reactions in chemistry and biochemistry.  He then was a Myron A. Bantrell postdoctoral fellow at Caltech with Professor Robert H. Grubbs where he studied titanocene methylenes as reagents in organic synthesis and the mechanism of Ziegler-Natta polymerization.  In 1984 he began as an assistant professor of chemistry MIT.  He was promoted to the associate professor (1989) and to Professor (1993) and was named the Camille Dreyfus Professor in 1997.  In July 2015, he became Associate Head of the Chemistry Department at MIT.  During his time at MIT he has received numerous honors including the Harold Edgerton Faculty Achievement Award of MIT, an Arthur C. Cope Scholar Award, the 2000 Award in Organometallic Chemistry from the American Chemical Society and a MERIT award from the National Institutes of Health.  He has also been the recipient of the Bristol-Myers Squibb Distinguished Achievement Award and the CAS Science Spotlight Award, both received in 2005 and the American Chemical Society's Award for Creative Work in Synthetic Organic Chemistry as well as the Siegfried Medal Award in Chemical Methods which Impact Process Chemistry, both received in 2006. In 2010 he received the Gustavus J. Esselen Award for Chemistry in the Public Interest. He received the 2013 Arthur C. Cope Award from the American Chemical Society. In 2014 he was the recipient of the Linus Pauling Medal Award and the Ulysses Medal (University College Dublin). In 2015 he received an honorary doctoral degree from the University of South Florida, and also received the BBVA Frontiers in Knowledge Award in Basic Sciences (2014 Award). He was recently selected to receive the 2016 William H. Nichols Medal. In 2000, he was elected as a fellow of the American Academy of Arts and Sciences and in 2008 he was elected as a member of the National Academy of Science. He is the coauthor of over 435 published or accepted papers and 47 issued patents.  He serves as a consultant to a number of companies and is an associate editor of Advanced Synthesis and Catalysis.

https://chemistry-buchwald.mit.edu/

Asymmetric Hydrofunctionalization Processes for Organic Synthesis
Abstract: The availability of a general method for the catalytic conversion of olefins into enantiomerically enriched amines has eluded chemists for decades. We have recently developed a simple copper- catalyzed technique to effect such a transformation. This lecture will describe our progress, applications of our methodology as well as our current view of the mechanism of the hydroamination process. In addition, we will describe our progress in developing new catalytic processes for carbon- carbon bond formation that utilize alkyl copper intermediates.
Timothy Curran - Vertex Pharmaceuticals



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Jamie McCabe Dunn - Merck


Jamie McCabe Dunn obtained her PhD from the University of Pittsburgh under the supervision of Kay Brummond, followed by a postdoctoral position at the University of Colorado in the group of Andrew Phillips. Jamie began her career at Merck in 2009 in the Union Process Chemistry group, where her impacts included endgame chemistry development for early GMP deliveries on the BACE (MK-8931) and diabetes programs that were successfully executed in the pilot plant. In 2010 Jamie undertook a new challenge in joining Merck Discovery Process Chemistry group, DPC, where her experience and impacts span the broad range of DPC activities that enable Merck’s early pipeline, such as developing novel chemistry to facilitate Medicinal Chemistry SAR, driving the critical early stage workflows and transitioning candidates into Development. In July 2017 Jamie joined the Process Chemistry group and has taken on the project lead role for a late stage neuroscience program

Accessing Novel Phosphoramidate Prodrugs via the Protecting-Group Free Selective 3’-Functionalization of Nucleosides

Abstract: Linear and cyclic phosphoramidate and phosphonate prodrugs are of growing importance in the development of novel HCV, HIV and oncology pro-nucleotide (ProTides) therapies. Much research in this area has focused on the development of direct, chemoselective or enantioselective reactions to provide 5’-ProTides. However, the development of a direct and efficient synthesis of 3’-ProTides, which was a key feature of our design to synthesize cyclic prodrugs, remained relatively unexplored. In an effort to develop an efficient, robust and scalable route to support Phase 1 clinical studies, we discovered a direct and chemoselective 3’-phosphoramidation that enabled the direct functionalization of the secondary hydroxyl group at the nucleoside 3’-position in the presence of the unprotected 5’-primary hydroxyl group. In addition to the successful application of this chemistry in GMP campaigns, the investigation of this rare selectivity was explored through a combination of NMR spectroscopy and computational studies. The findings of these studies allowed us to develop a predictive computational model that accurately assesses the potential for 3’-functionalization for a broad range of nucleosides and nucleoside mimetics. The discovery, development and delivery of a cyclic ProTide, as well as the understanding the selectivity and demonstration of the method on a broad scope of nucleosides and electrophiles will be presented.

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Steven Mennen - Amgen
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Sarah Reisman - California Institute of Technology

Sarah E. Reisman conducted undergraduate studies at Connecticut College in New London, CT, where she became interested in organic synthesis working in the laboratory of Prof. Timo Ovaska. After receiving her BA in Chemistry in 2001, Sarah enrolled in graduate studies at Yale University and joined the research group of Prof. John Wood. She earned her Ph.D. in chemistry in 2006, conducting research in the area of natural product synthesis. As an NIH post-doctoral fellow, Sarah pursued studies in the field of asymmetric catalysis working with Prof. Eric Jacobsen at Harvard University. In 2008, Sarah joined the faculty at the California Institute of Technology where she is now a Professor of Chemistry. Her laboratory seeks to discover, develop, and study new chemical reactions within the context of natural product total synthesis. Prof. Reisman has been recognized with a number of awards for teaching and research, including an Alfred P. Sloan Research Fellowship, Arthur C. Cope Scholar Award, the Amgen Young Investigator Award, the Novartis Early Career Award, and the Bristol-Myers Squibb Unrestricted Grant in Synthetic Organic Chemistry.


http://reismangroup.caltech.edu/

Necessity is the Mother of Invention: Natural Products and the Chemistry They Inspire

Abstract: The chemical synthesis of natural products provides an exciting platform from which to conduct fundamental research in chemistry and biology. Our group is currently pursuing the synthesis of a number of structurally complex natural products, including the diterpenoid alkaloid talatisamine and the antibiotic pleuromutilin. The densely-packed arrays of heteroatoms and stereogenic centers that constitute these polycyclic targets challenge the limits of current technology and inspire the development of new synthetic strategies and tactics. This seminar will describe the latest progress in our methodological and target-directed synthesis endeavors.

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Richmond Sarpong - University of California, Berkeley

http://www.cchem.berkeley.edu/rsgrp/

Strategies and Methods for Chemical Synthesis Inspired by Natural Products


Abstract: Natural products continue to inspire and serve as the basis of new medicines. They also provide intricate problems that expose limitations in the strategies and methods employed in chemical synthesis. Several strategies and methods that have been developed in our laboratory and applied to the syntheses of architecturally complex diterpenoid alkaloids, indole alkaloids, and several Lycopodium alkaloids, will be presented and discussed.

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Corinna Schindler - University of Michigan

https://www.schindlerresearchgroup.com/

Iron(III)-Catalyzed Carbonyl-Olefin Metathesis
The metathesis reaction between two unsaturated organic substrates is one of organic chemistry’s most powerful carbon-carbon bond forming reactions. The catalytic olefin-olefin metathesis reaction has led to profound developments in the synthesis of molecules relevant to the petroleum, materials and pharmaceutical industries. These reactions are characterized by their use of discrete metal alkylidene catalysts that operate by a well-established reaction mechanism. While the corresponding carbonyl-olefin metathesis reaction similarly enables the direct construction of carbon-carbon bonds, currently available methods are scarce and hampered by either harsh reaction conditions or the requirement of stoichiometric transition metal complexes as reagents. We have recently developed the first catalytic carbonyl-olefin ring-closing metathesis reaction that utilizes iron as an earth-abundant and environmentally benign transition metal.
[1], [2] Our reaction design accommodates a variety of substrates and is distinguished by its operational simplicity, mild reaction conditions, high functional group tolerance, and amenability to gram scale synthesis.[3]
Jim Yang - Biogen
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