SUNDAY |
2:00 pm - 9:00 pm | Arrival and Check-in (Office Closed 6:00 pm - 7:00 pm) |
6:00 pm | Dinner |
7:30 pm - 7:40 pm | Welcome / Introductory Comments by GRC Site Staff |
7:40 pm - 9:30 pm | New Strategies for Heterocycle Synthesis I |
| Discussion Leader: John Wood (Vice Chair,Colorado State University) |
7:40 pm - 8:20 pm | Mark Lautens (University of Toronto)
"No Strain, No Gain? Lessons in Catalysis"
|
8:20 pm - 8:30 pm | Discussion |
8:30 pm - 8:40 pm | Jared Shaw (University of California, Davis)
"Multicomponent Reactions and Tandem Processes for the Synthesis of Complex Heterocycles" |
8:40 pm - 8:45 pm | Discussion |
8:45 pm - 9:25 pm | Erick Carriera (ETH Zurich)
"Surpises and Discovery with Heterocycles"
|
9:25 pm - 9:30 pm | Discussion |
MONDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Catalysis in Heterocycle Synthesis |
| Discussion Leader: Hien Nguyen (University of Iowa) |
9:00 am - 9:40 am | Tamejiro Hiyama (Kyoto University)
"Post Cross-Coupling Approach for Conjugated Heterocycles"
|
9:40 am - 9:50 am | Discussion |
9:50 am - 10:20 am | Group Photo / Coffee Break |
10:20 am - 11:10 am | Sherry Chemler (University at Buffalo)
"Copper-catalyzed enantioselective heterocycle synthesis"
|
11:10 am - 11:20 am | Discussion |
11:20 am - 11:40 am | Daniel. J. Weix (University of Rochester)
"Nucleophile-Free Cross-Coupling: Mechanism and Scope" |
11:40 am - 11:45 am | Discussion |
11:45 am - 12:20 pm | Huan Wang (Glaxosmithkline)
"Ring Closing Metathesis in the Synthesis of SB462795: Reduction of Catalyst Loading"
|
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 #1 (Convenor John Wood, Vice Chair) |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Heterocyclic Natural Products |
| Discussion Leader: Sheila Hauck (AstraZeneca) |
7:30 pm - 8:10 pm | Jim Anderson (UCL, UK)
"New Heterocycles using 1,2-Diamines from the Nitro-Mannich Reaction" |
8:10 pm - 8:30 pm | Discussion |
8:30 pm - 9:10 pm | William Roush (The Scripps Research Institute, Florida)
"Synthesis of Bifunctional Allylboron Reagents via Allene Hydroboration Reactions and Applications to the Synthesis of Biologically Active Natural Products"
|
9:10 pm - 9:30 pm | Discussion |
TUESDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Biological Aspects of Heterocyclic Chemistry |
| Discussion Leader: Mark Behnke (National Institutes of Health) |
9:00 am - 9:35 am | Shuang Liu (Albany Molecular Research)
"The Discovery of Novel Triple Reuptake Inhibitors" |
9:35 am - 9:45 am | Discussion |
9:45 am - 10:25 am | Dennis Dougherty (Caltech)
"The Cation-π Interaction in Chemistry and Biology" |
10:25 am - 10:35 am | Discussion |
10:35 am - 11:05 am | Coffee Break |
11:05 am - 11:35 am | Chong Han (Genentech)
"Process Chemistry Development on the AKT Inhibitor GDC-0068: Enabling Uninterrupted Clinical Supply"
|
11:35 am - 11:45 am | Discussion |
11:45 am - 12:20 pm | Thomas J. Beauchamp (Eli Lilly)
"A Selective Route into 1,2,3-Triazoles via the Use of the Silicon beta-effect" |
12:20 pm - 12:30 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 6:00 pm | Free Time |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | New Strategies for Heterocycle Synthesis |
| Discussion Leader: Daniel Elbaum (Pfizer) |
7:30 pm - 8:10 pm | Tomislav Rovis (Colorado State University)
"Design and Utility of Chiral Carbenes for Asymmetric Umpolung"
|
8:10 pm - 8:20 pm | Discussion |
8:20 pm - 8:35 pm | Scott Bagley (Pfizer)
"Synthetic Strategies for Spiro-Heterocyclic ACC Inhibitors" |
8:35 pm - 8:40 pm | Discussion |
8:40 pm - 9:20 pm | Armido Studer (University of Munster, Germany)
"Nitroxides as mild oxidants in synthesis"
|
9:20 pm - 9:30 pm | Discussion |
WEDNESDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Advances in the Synthesis of Heterocyclic Compounds |
| Discussion Leader: Scott Sutton (Pfizer) |
9:00 am - 9:40 am | Tim Gallagher (University of Bristol, UK)
"Exploring Cytisine"
|
9:40 am - 9:50 am | Discussion |
9:50 am - 10:30 am | David Chen (Seoul National University, South Korea)
"Strategies and Opportunities in the Synthesis of Heterocyclic Natural Products"
|
10:30 am - 10:40 am | Discussion |
10:40 am - 10:50 am | Business Meeting, Part I |
| Nominations for the next Vice Chair |
10:50 am - 11:10 am | Coffee Break |
11:10 am - 11:40 am | Norito Takenaka (University of Miami)
"Asymmetric Catalysis with Helical-Chiral Pyridines"
|
11:40 am - 11:45 am | Discussion |
11:45 am - 12:20 pm | Yi-Yin Ku (Abbott)
"Development of an Enabling Large Scale Synthesis of an a Potent and Selective HCV Polymerase 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 #2 (Convenor John Wood, Vice Chair) |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Target synthesis in Heterocyclic Chemistry |
| Discussion Leader: Stacey E. Brenner-Moyer (The City University of New York at Brooklyn College) |
7:30 pm - 8:10 pm | David Black (University of New South Wales, Australia)
"Macrocyclic Tetraindolyls: Indorphyrins and related structures as potential new foundation molecules"
|
8:10 pm - 8:20 pm | Discussion |
8:20 pm - 8:35 pm | Sebastien Caille (Amgen)
"Catalytic Asymmetric Synthesis of a Tertiary Benzylic Carbon Center via Phenol-Directed Alkene Hydrogenation" |
8:35 pm - 8:40 pm | Discussion |
8:40 pm - 9:20 pm | John H. Freudenberger (Dupont)
"Preparation of 3-Halo-1-Aryl-1H-Pyrazole-5-Carboxylic Acids: The Early Process Development of Rynaxypyr™"
|
9:20 pm - 9:30 pm | Discussion |
THURSDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Mechanisms in Heterocyclic Chemistry |
| Discussion Leader: Chris Grote (Covidien) |
9:00 am - 9:40 am | Donna Blackmond (Scripps)
"Mechanistic Studies in Pyrrolidine-Based Organocatalysis"
|
9:40 am - 9:50 am | Discussion |
9:50 am - 10:25 am | Matthew L. Maddess (Merck)
"Process Development and Delivery of a Selective Estrogen Receptor Beta Agonist" |
10:25 am 10:35 am | Discussion |
10:35 am - 11:05 am | Business Meeting, Part II |
| Fill out Conference Evaluation Forms; Discuss future Site & Scheduling preferences; Election of the next Vice Chair |
11:05 am - 11:35 am | Coffee Break |
11:35 am - 12:15 pm | Guy Lloyd-Jones (University of Bristol UK)
"Amides and Esters"
|
12:15 pm - 12:25 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 6:00 pm | Free Time |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | New Reactions in Heterocycle Synthesis |
| Discussion Leader: Diane Carrera (Genetech) |
7:30 pm - 8:10 pm | Paul Murray (Cat.Sci)
"General Catalytic Protocols for the synthesis of Complex Drug Molecules" |
8:10 pm - 8:30 pm | Discussion |
8:30 pm - 9:10 pm | David MacMillan (Princeton)
"Multi Catalysis in Chemical Synthesis" |
9:10 pm - 9:20 pm | Discussion |
9:20 pm - 9:30 pm | Closing Remarks (Vice Chair) |
FRIDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am | Departure |