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 | Synthesis of Heterocyclic Natural Products - Transformation |
| Discussion Leader: James Leahy (University of South Florida, USA) |
7:40 pm - 7:55 pm | Opening Remarks |
7:55 pm - 8:25 pm | Viresh Rawal (University of Chicago, USA) "Recent Progress in the Total Synthesis of Indole
Alkaloids" |
8:25 pm - 8:35 pm | Discussion |
8:35 pm - 8:45 pm | Maciej Walczak (University of Colorado, USA) "Synthesis of Saturated Nitrogen Heterocycles via Catalytic Reduction with Phosphorus-NHC Complexes" |
8:45 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Daniel Romo (Texas A&M University, USA) "Heterocycles via Unsaturated Acyl Ammonium Salts:
Applications to Natural Products" |
9:20 pm - 9:30 pm | Discussion |
Monday |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Heterocyclic Reactions and Catalysis |
| Discussion Leader: James Stambuli (AbbVie, USA) |
9:00 am - 9:30 am | Laszlo Kurti (Rice University, USA) "Exploiting the Versatile N-O Bond: Rapid Synthesis of
N- and O-Heterocycles" |
9:30 am - 9:40 am | Discussion |
9:40 am - 9:50 am | Paul Keller (University of Wollongong, Australia) "Twisting by the Chiral Pool: Helical DiPnictogen Ligands 'Made Easy'" |
9:50 am - 9:55 am | Discussion |
9:55 am - 10:10 am | Andrew McClory (Genentech, Inc., USA) "PIM Inhibitor GDC-0339: First Generation cGMP Process Chemistry Route" |
10:10 am - 10:20 am | Discussion |
10:20 am - 10:50 am | Coffee Break |
10:50 am - 11:20 am | Janis Louie (University of Utah, USA) "Advances in Ni- and Fe-Catalyzed Cycloaddition
Chemistry" |
11:20 am - 11:30 am | Discussion |
11:30 am - 11:40 am | Catharine Larsen (University of California, Riverside, USA) "Alpha-Tetra Substituted Nitrogen Heteroaromatics: Quinolines and Triazoles" |
11:40 am - 11:45 am | Discussion |
11:45 am - 12:20 pm | David Lupton (Monash University, Australia) "N-Heterocyclic Carbene Catalysis with Esters and
Activated Acids" |
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 - Ascendance |
| Discussion Leader: Corinna Schindler (University of Michigan, USA) |
7:30 pm - 8:00 pm | Patrick Harran (University of California, Los Angeles, USA) "A Fresh Look at Complex Prodiginines" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Minoru Isobe (National Sun Yat-Sen University, Taiwan) "Cobalt-Assisted Ring Cyclization" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:25 pm | Albert Padwa (Emory University, USA) "A 50 Year Infatuation/Obsession with 1,3-Dipoles" |
9:25 pm - 9:30 pm | Discussion |
Tuesday |
7:30 am - 8:30 am | Breakfast |
8:30 am | Group Photo |
9:00 am - 12:30 pm | Innovative Solutions |
| Discussion Leader: Catharine Larsen (University of California, Riverside, USA) |
9:00 am - 9:30 am | Jeffrey Katz (Colby College, USA) "Acetylene-Activated SNAr Reactions for Heterocycle and
Macrocycle Synthesis" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Julia Clay (Eli Lilly & Co., USA) "For Scientists by Scientists: Lilly’s Open Innovation Drug Discovery Program" |
10:10 am - 10:20 am | Discussion |
10:20 am - 10:50 am | Coffee Break |
10:50 am - 11:00 am | Joshua Pierce (North Carolina State University, USA) "Marine Natural Products Synthesis: A Platform for Chemical and Biological Discovery" |
11:00 am - 11:05 am | Discussion |
11:05 am - 11:35 am | Jared Shaw (University of California, Davis, USA) "Complex Heterocycles from Multicomponent Reactions and Asymmetric Catalysis" |
11:35 am - 11:45 am | Discussion |
11:45 am - 12:20 pm | Michael Sherburn (Australian National University, Australia) "Heterocycle Synthesis: Lean and Mean with a Polyene" |
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 | Discovery: Marine-Derived Heterocycles |
| Discussion Leader: Frank Fang (Eisai, USA) |
7:30 pm - 8:00 pm | Kirk Gustafson (National Cancer Institute, NIH, USA) "Novel Bioactive Heterocyclic Scaffolds from Marine
Invertebrates: Intriguing New
Compounds and the Structural Elucidation Challenges They Present" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Frank Fang (Eisai, USA) "Synthesis of Heterocyclic Marine Natural Product-Based
Therapeutics" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:25 pm | Carmen Cuevas (PharmaMar, Spain) "Marine Payloads for New ADCs" |
9:25 pm - 9:30 pm | Discussion |
Wednesday |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Heterocycles and Contemporary Therapeutics |
| Discussion Leader: Colin Skepper (Novartis, USA) |
9:00 am - 9:30 am | Eric Voight (AbbVie, USA) "Heterocycle Synthesis at the Interface Between
Discovery and Process Chemistry" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Michael Kernan (Gilead Sciences, USA) "Development of Heterocyclic Compounds as Treatments for Antiviral Diseases" |
10:10 am - 10:20 am | Discussion |
10:20 am - 10:50 am | Coffee Break |
10:50 am - 11:05 am | Louis Barriault (University of Ottawa, Canada) "New Opportunities in Natural Products Synthesis Using Phosphino Gold(I) Catalyst" |
11:05 am - 11:10 am | Discussion |
11:10 am - 11:40 am | Nga Do (Pfizer, USA) "Warp Speed Development, Filing and Approval of Palbociclib" |
11:40 am - 11:50 am | Discussion |
11:50 am - 12:20 pm | Kyle Eastman (Bristol-Myers Squibb, USA) "The Evolution of HCV NS5B Site II Inhibitors: A Template, a Clinical Candidate and a Pan-Genotype Inhibitor" |
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 | Synthetic Methodology |
| Discussion Leader: Kami Hull (University of Illinois at Urbana-Champaign, USA) |
7:30 pm - 8:00 pm | Pavel Nagorny (University of Michigan, USA) "New Methods for the Synthesis of Natural Products" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Jennifer Stockdill (Wayne State University, USA) "Enabling Reactivity of Neutral Aminyl Radicals in
Polycyclic Heterocycle Synthesis" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Robert Knowles (Princeton University, USA) "Proton-Coupled Electron Transfer in Organic Synthesis
and Asymmetric Catalysis" |
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 | Tools, Solutions and Pathways to New Therapeutics |
| Discussion Leader: Seble Wagaw (AbbVie, USA) |
9:00 am - 9:30 am | Qiu Wang (Duke University, USA) "Uncapping the Potential of Electrophilic Amination in
the Functionalizations of C-H Bonds and Olefins" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Lisa Marcaurelle (H3 Biomedicine, USA) "Diversity-Oriented Synthesis for Oncology Drug Discovery" |
10:10 am - 10:20 am | Discussion |
10:20 am - 10:50 am | Coffee Break |
10:50 am - 11:00 am | Andrew Lawrence (University of Edinburgh, United Kingdom) "Biomimetic Synthesis of Dimeric Natural Products" |
11:00 am - 11:05 am | Discussion |
11:05 am - 11:35 am | Shiping Xie (GlaxoSmithKline, USA) "Conversion of a Benzofuran Ester to an Amide Through an Enamine Lactone Pathway: Efficient Synthesis of HCV Polymerase Inhibitor GSK852A" |
11:35 am - 11:45 am | Discussion |
11:45 am - 12:20 pm | John MacMillan (University of Texas Southwestern Medical Center, USA) "Expanding Natural Product Diversity from Microorganisms by Exploitation of Non-Enzymatic Transformations" |
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: Synthesis and Biosynthesis of Heterocyclic Natural Products |
| Discussion Leader: Jared Shaw (University of California, Davis, USA) |
7:30 pm - 7:35 pm | Introduction by Discussion Leader |
7:35 pm - 8:15 pm | James Panek (Boston University, USA) "Advances in the Stereocontrolled Synthesis of Complex
Natural Products" |
8:15 pm - 8:25 pm | Discussion |
8:25 pm - 9:05 pm | Robert Williams (Colorado State University, USA) "Synthesis and Biosynthesis of Heterocyclic Ring Systems in Natural Products Derived from Marine and Terrestrial Fungi" |
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 |