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Heterocyclic Compounds
Gordon Research Conference

New Reactions, Innovation and Creative Design in the Synthesis and Applications of Heterocyclic Compounds

Dates

June 19-24, 2016

Location

Salve Regina University
Newport, RI

Organizers

Chair:
Scott C. Sutton

Vice Chair:
Daniel Romo

Meeting Description

The synthesis of heterocyclic compounds continues to attract enthusiastic endeavors designed to push the boundaries of what some have considered a mature field. Arguably, the boundaries of heterocyclic chemistry are limited only by ones' imagination. Heterocyclic compounds constitute the largest and most varied family of organic compounds with utility spanning photography to pharmaceuticals and beyond. New synthetic methods for heterocycle synthesis surface each month and are a testament to the rapid growth in this field. In fact, we are witness to the burgeoning growth of a field that has transformed society through spectacular innovations, implemented through applications of heterocycles in arenas spanning material science to new therapeutics for the treatment of cancer. The 2016 Heterocyclic Compounds GRC offers a contemporary look into state-of-the-art synthetic methods and a portico view of future directions and trends. At this conference, an extraordinary schedule of domestic and international speakers and an impressive lineup of posters will highlight recent advances in this field. Highlighted topics include heterocycles as redox mediators in organic electrochemistry, transition metal catalysis, natural product synthesis and heterocycles as the backbone of drug discovery. Please join us at this GRC for one of the most scientifically rich conferences of the year.

Contributors

Final Meeting Program

Sunday
2:00 pm - 9:00 pmArrival and Check-in
6:00 pmDinner
7:30 pm - 7:40 pmWelcome / Introductory Comments by GRC Site Staff
7:40 pm - 9:30 pmNew Methods for the Synthesis of Heterocyclic Compounds
Discussion Leader: Mark Behnke (TRND, National Center for Advancing Translational Sciences, NIH, USA)
7:40 pm - 7:55 pmOpening Remarks
7:55 pm - 8:25 pmGojko Lalic (University of Washington, USA)
"Copper Catalysis in Hydrofunctionalization of Unsaturated Compounds"
8:25 pm - 8:35 pmDiscussion
8:35 pm - 9:20 pmAndrei Yudin (University of Toronto, Canada)
"Discovery and Development of Bioactive Molecules Using the Tools of Heterocyclic Chemistry"
9:20 pm - 9:30 pmDiscussion
Monday
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmCatalysis in Heterocyclic Chemistry
Discussion Leader: Catharine Larsen (University of California, Riverside, USA)
9:00 am - 9:30 amMary Watson (University of Delaware, USA)
"Enantioselective, Copper-Catalyzed Alkynylations of Oxocarbenium and Iminium Ions"
9:30 am - 9:40 amDiscussion
9:40 am - 10:25 amSherry Chemler (State University of New York at Buffalo, USA)
"Stereoselective Copper-Catalyzed Saturated Heterocycle Synthesis"
10:25 am - 10:35 amDiscussion
10:35 am - 11:05 amCoffee Break
11:05 am - 11:25 amChad Eichman (Loyola University Chicago, USA)
"Catalytic Bisfunctionalizations of Unsaturated Compounds for Heterocycle Synthesis"
11:25 am - 11:35 amDiscussion
11:35 am - 12:20 pmGuangbin Dong (The University of Chicago, USA)
"Hetero- and Carbocycle Formation via C-C Activation of Ketones"
12:20 pm - 12:30 pmDiscussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session
6:00 pmDinner
7:30 pm - 9:30 pmSynthesis of Heterocyclic Natural Products
Discussion Leader: Sherry Chemler (State University of New York at Buffalo, USA)
7:30 pm - 7:55 pmRegan Thomson (Northwestern University, USA)
"Modular Approaches to the Synthesis of Polycyclic Natural Products"
7:55 pm - 8:05 pmDiscussion
8:05 pm - 8:30 pmThomas Maimone (University of California, Berkeley, USA)
"Synthetic Studies Toward Complex Natural Products"
8:30 pm - 8:40 pmDiscussion
8:40 pm - 9:20 pmNeil Garg (University of California, Los Angeles, USA)
"Recent Studies in Methods Development and Complex Molecule Synthesis"
9:20 pm - 9:30 pmDiscussion
Tuesday
7:30 am - 8:30 amBreakfast
8:30 amGroup Photo
9:00 am - 12:30 pmRoute Optimization of Biologically Active Heterocyles
Discussion Leader: Daniel Fandrick (Boehringer Ingelheim Pharmaceuticals, Inc., USA)
9:00 am - 9:30 amSebastien Caille (Amgen, USA)
"A Telescoped Process to Manufacture 6,6,6-Trifluorofucose, an Inhibitor of Fucosylation Utilized in Monoclonal Antibody Production"
9:30 am - 9:40 amDiscussion
9:40 am - 10:10 amLakshmaiah Gingipalli (AstraZeneca, USA)
"Expedient Solid Phase Synthesis of Tubulysin Analogs with Potential Applications in Oncology"
10:10 am - 10:20 amDiscussion
10:20 am - 10:50 amCoffee Break
10:50 am - 11:30 amLouis-Charles Campeau (Merck Research Laboratories, USA)
"Discovery and Development of Novel Reactions in the Manufacturing of Heterocyclic Therapeutic Agents"
11:30 am - 11:40 amDiscussion
11:40 am - 12:20 pmErick Carreira (ETH Zurich, Switzerland)
"Recent Advances in Asymmetric Catalytic Synthesis of Heterocycles"
12:20 pm - 12:30 pmDiscussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session
6:00 pmDinner
7:30 pm - 9:30 pmInsights into the Biosynthesis of Heterocyclic Natural Products
Discussion Leader: Jason Herr (Albany Molecular Research, Inc. (AMRI), USA)
7:30 pm - 8:00 pmAndrei Kutateladze (University of Denver, USA)
"Photoassisted Synthesis of Complex Polyheterocyclic Molecular Architectures"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:35 pmDebra Wallace (Merck and Co., USA)
"The Importance of Mechanistic Understanding for Reaction Optimization"
8:35 pm - 8:45 pmDiscussion
8:45 pm - 9:20 pmCraig Williams (University of Queensland, Australia)
"Pursuing Complex Diterpene Isolation and Total Syntheses"
9:20 pm - 9:30 pmDiscussion
Wednesday
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmNew Strategies to Construct Heterocyclic Compounds
Discussion Leader: Cynthia Shafer (Novartis Institutes for Biomedical Research, USA)
9:00 am - 9:30 amIan Baxendale (Durham University, United Kingdom)
"Evaluating the Benefits of Flow Chemistry for Heterocyclic Synthesis"
9:30 am - 9:40 amDiscussion
9:40 am - 10:00 amDipannita Kalyani (St. Olaf College, USA)
"Pd- and Ni-Catalyzed Synthesis of Heterocyclic Scaffolds"
10:00 am - 10:10 amDiscussion
10:10 am - 10:40 amCoffee Break
10:40 am - 11:00 amDavid Michaelis (Brigham Young University, USA)
"Enantioselective Heterocycle Synthesis with Ti-M Heterobimetallic Catalysts"
11:00 am - 11:10 amDiscussion
11:10 am - 11:40 amWilliam Chain (University of Delaware, USA)
"Synthetic Methods Inspired by Terpenoid and Alkaloid Natural Products"
11:40 am - 11:50 amDiscussion
11:50 am - 12:20 pmDaniel Little (University of California, Santa Barbara, USA)
"Application of Some Basic Principles of Electroorganic Synthesis to the Assembly of Heterocycles"
12:20 pm - 12:30 pmDiscussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session
6:00 pmDinner
7:30 pm - 9:30 pmDesign and Synthesis of Biologically Active Heterocyclic Compounds
Discussion Leader: Eric Voight (AbbVie, USA)
7:30 pm - 8:00 pmPeter Dragovich (Genentech, USA)
"Influence of Heterocycle Structure on NAMPT Inhibitor Biological Activity: Cell Potency and CYP Inhibition"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:40 pmPrabhakar Jadhav (Eli Lilly and Company, USA)
"Transdermal Selective Androgen Receptor Modulator (SARM) for Muscle Atrophy"
8:40 pm - 8:50 pmDiscussion
8:50 pm - 9:20 pmMaurice Marsini (Boehringer Ingelheim Pharmaceuticals, Inc., USA)
"Development of a Concise, Scalable Synthesis of a Heterocyclic CCR1 Antagonist Utilizing a Continuous Flow Curtius Rearrangement"
9:20 pm - 9:30 pmDiscussion
Thursday
7:30 am - 8:30 amBreakfast
8:30 am - 9:00 amBusiness Meeting
Nominations for the Next Vice Chair; Fill in Conference Evaluation Forms; Discuss Future Site and Scheduling Preferences; Election of the Next Vice Chair
9:00 am - 12:30 pmHeterocyles as Tools Impacting the Study of Human Disease
Discussion Leader: Jennifer Roizen (Duke University, USA)
9:00 am - 9:15 amSusan Meschwitz (Salve Regina University, USA)
"Design and Synthesis of Pyrazinones and Pyrimidinones as Anti-Virulence Agents"
9:15 am - 9:25 amDiscussion
9:25 am - 9:50 amDmitry Tsvelikhovsky (The Hebrew University of Jerusalem, Israel)
"Rapid Composition of Tricyclic Spiranoid Lactones: Regio- and Stereoselective Access to Natural and Unexplored Frames"
9:50 am - 10:00 amDiscussion
10:00 am - 10:30 amCoffee Break
10:30 am - 11:00 amYoula Tsantrizos (McGill University, Canada)
"Synthesis of Phosphorus-Containing Heterocyclic Compounds as Leads for Drug Discovery and as Tools for Metal-Mediated Catalysis"
11:00 am - 11:10 amDiscussion
11:10 am - 11:40 amGisele Nishiguchi (Novartis, USA)
"Discovery of Clinical Candidate PIM447, a Potent and Selective Pan-PIM Inhibitor for the Treatment of Hematological Malignancies"
11:40 am - 11:50 amDiscussion
11:50 am - 12:20 pmSarah O'Connor (John Innes Centre, United Kingdom)
"How Plants Synthesize Heterocycles"
12:20 pm - 12:30 pmDiscussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session
6:00 pmDinner
7:30 pm - 9:30 pmKeynote Session: Perspectives on Heterocyclic Chemistry
Discussion Leader: Qiu Wang (Duke University, USA)
7:30 pm - 8:10 pmRobert Singer (Pfizer Inc, USA)
"Asymmetric Synthesis of a Gamma Secretase Inhibitor with Biocatalysis"
8:10 pm - 8:20 pmDiscussion
8:20 pm - 9:05 pmJohn Hartwig (University of California, Berkeley, USA)
"Transition Metal-Catalyzed Reactions for the Synthesis and Modification of Heterocycles"
9:05 pm - 9:15 pmDiscussion
9:15 pm - 9:30 pmClosing Remarks
Friday
7:30 am - 8:30 amBreakfast
9:00 amDeparture
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