Sunday |
2:00 pm - 9:00 pm | Arrival and Check-in |
6:00 pm | Dinner |
7:30 pm - 7:40 pm | Welcome / Introductory Comments by GRC Site Staff |
7:40 pm - 9:30 pm | New 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 pm | Opening Remarks |
7:55 pm - 8:25 pm | Gojko Lalic (University of Washington, USA) "Copper Catalysis in Hydrofunctionalization of Unsaturated Compounds" |
8:25 pm - 8:35 pm | Discussion |
8:35 pm - 9:20 pm | Andrei Yudin (University of Toronto, Canada) "Discovery and Development of Bioactive Molecules Using the Tools of Heterocyclic Chemistry" |
9:20 pm - 9:30 pm | Discussion |
Monday |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Catalysis in Heterocyclic Chemistry |
| Discussion Leader: Catharine Larsen (University of California, Riverside, USA) |
9:00 am - 9:30 am | Mary Watson (University of Delaware, USA) "Enantioselective, Copper-Catalyzed Alkynylations of Oxocarbenium and Iminium Ions" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:25 am | Sherry Chemler (State University of New York at Buffalo, USA) "Stereoselective Copper-Catalyzed Saturated Heterocycle Synthesis" |
10:25 am - 10:35 am | Discussion |
10:35 am - 11:05 am | Coffee Break |
11:05 am - 11:25 am | Chad Eichman (Loyola University Chicago, USA) "Catalytic Bisfunctionalizations of Unsaturated Compounds for Heterocycle Synthesis" |
11:25 am - 11:35 am | Discussion |
11:35 am - 12:20 pm | Guangbin Dong (The University of Chicago, USA) "Hetero- and Carbocycle Formation via C-C Activation of Ketones" |
12:20 pm - 12:30 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 4:00 pm | Free Time |
4:00 pm - 6:00 pm | Poster Session |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Synthesis of Heterocyclic Natural Products |
| Discussion Leader: Sherry Chemler (State University of New York at Buffalo, USA) |
7:30 pm - 7:55 pm | Regan Thomson (Northwestern University, USA) "Modular Approaches to the Synthesis of Polycyclic Natural Products" |
7:55 pm - 8:05 pm | Discussion |
8:05 pm - 8:30 pm | Thomas Maimone (University of California, Berkeley, USA) "Synthetic Studies Toward Complex Natural Products" |
8:30 pm - 8:40 pm | Discussion |
8:40 pm - 9:20 pm | Neil Garg (University of California, Los Angeles, USA) "Recent Studies in Methods Development and Complex Molecule Synthesis" |
9:20 pm - 9:30 pm | Discussion |
Tuesday |
7:30 am - 8:30 am | Breakfast |
8:30 am | Group Photo |
9:00 am - 12:30 pm | Route Optimization of Biologically Active Heterocyles |
| Discussion Leader: Daniel Fandrick (Boehringer Ingelheim Pharmaceuticals, Inc., USA) |
9:00 am - 9:30 am | Sebastien 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 am | Discussion |
9:40 am - 10:10 am | Lakshmaiah Gingipalli (AstraZeneca, USA) "Expedient Solid Phase Synthesis of Tubulysin Analogs with Potential Applications in Oncology" |
10:10 am - 10:20 am | Discussion |
10:20 am - 10:50 am | Coffee Break |
10:50 am - 11:30 am | Louis-Charles Campeau (Merck Research Laboratories, USA) "Discovery and Development of Novel Reactions in the Manufacturing of Heterocyclic Therapeutic Agents" |
11:30 am - 11:40 am | Discussion |
11:40 am - 12:20 pm | Erick Carreira (ETH Zurich, Switzerland) "Recent Advances in Asymmetric Catalytic Synthesis of Heterocycles" |
12:20 pm - 12:30 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 4:00 pm | Free Time |
4:00 pm - 6:00 pm | Poster Session |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Insights into the Biosynthesis of Heterocyclic Natural Products |
| Discussion Leader: Jason Herr (Albany Molecular Research, Inc. (AMRI), USA) |
7:30 pm - 8:00 pm | Andrei Kutateladze (University of Denver, USA) "Photoassisted Synthesis of Complex Polyheterocyclic Molecular Architectures" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:35 pm | Debra Wallace (Merck and Co., USA) "The Importance of Mechanistic Understanding for Reaction Optimization" |
8:35 pm - 8:45 pm | Discussion |
8:45 pm - 9:20 pm | Craig Williams (University of Queensland, Australia) "Pursuing Complex Diterpene Isolation and Total Syntheses" |
9:20 pm - 9:30 pm | Discussion |
Wednesday |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | New Strategies to Construct Heterocyclic Compounds |
| Discussion Leader: Cynthia Shafer (Novartis Institutes for Biomedical Research, USA) |
9:00 am - 9:30 am | Ian Baxendale (Durham University, United Kingdom) "Evaluating the Benefits of Flow Chemistry for Heterocyclic Synthesis" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:00 am | Dipannita Kalyani (St. Olaf College, USA) "Pd- and Ni-Catalyzed Synthesis of Heterocyclic Scaffolds" |
10:00 am - 10:10 am | Discussion |
10:10 am - 10:40 am | Coffee Break |
10:40 am - 11:00 am | David Michaelis (Brigham Young University, USA) "Enantioselective Heterocycle Synthesis with Ti-M Heterobimetallic Catalysts" |
11:00 am - 11:10 am | Discussion |
11:10 am - 11:40 am | William Chain (University of Delaware, USA) "Synthetic Methods Inspired by Terpenoid and Alkaloid Natural Products" |
11:40 am - 11:50 am | Discussion |
11:50 am - 12:20 pm | Daniel 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 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 4:00 pm | Free Time |
4:00 pm - 6:00 pm | Poster Session |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Design and Synthesis of Biologically Active Heterocyclic Compounds |
| Discussion Leader: Eric Voight (AbbVie, USA) |
7:30 pm - 8:00 pm | Peter Dragovich (Genentech, USA) "Influence of Heterocycle Structure on NAMPT Inhibitor Biological Activity: Cell Potency and CYP Inhibition" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Prabhakar Jadhav (Eli Lilly and Company, USA) "Transdermal Selective Androgen Receptor Modulator (SARM) for Muscle Atrophy" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Maurice 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 pm | Discussion |
Thursday |
7:30 am - 8:30 am | Breakfast |
8:30 am - 9:00 am | Business 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 pm | Heterocyles as Tools Impacting the Study of Human Disease |
| Discussion Leader: Jennifer Roizen (Duke University, USA) |
9:00 am - 9:15 am | Susan Meschwitz (Salve Regina University, USA) "Design and Synthesis of Pyrazinones and Pyrimidinones as Anti-Virulence Agents" |
9:15 am - 9:25 am | Discussion |
9:25 am - 9:50 am | Dmitry 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 am | Discussion |
10:00 am - 10:30 am | Coffee Break |
10:30 am - 11:00 am | Youla 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 am | Discussion |
11:10 am - 11:40 am | Gisele 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 am | Discussion |
11:50 am - 12:20 pm | Sarah O'Connor (John Innes Centre, United Kingdom) "How Plants Synthesize Heterocycles" |
12:20 pm - 12:30 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 4:00 pm | Free Time |
4:00 pm - 6:00 pm | Poster Session |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Keynote Session: Perspectives on Heterocyclic Chemistry |
| Discussion Leader: Qiu Wang (Duke University, USA) |
7:30 pm - 8:10 pm | Robert Singer (Pfizer Inc, USA) "Asymmetric Synthesis of a Gamma Secretase Inhibitor with Biocatalysis" |
8:10 pm - 8:20 pm | Discussion |
8:20 pm - 9:05 pm | John Hartwig (University of California, Berkeley, USA) "Transition Metal-Catalyzed Reactions for the Synthesis and Modification of Heterocycles" |
9:05 pm - 9:15 pm | Discussion |
9:15 pm - 9:30 pm | Closing Remarks |
Friday |
7:30 am - 8:30 am | Breakfast |
9:00 am | Departure |