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Heterocyclic Compounds
June 24-29, 2012
Salve Regina University
Newport, RI
Chair:
David C. Lathbury

Vice Chair:
John L. Wood

The first Heterocyclic compounds meeting was held in 1964, making it one of the longest running Gordon Research Conferences. This success and longevity is a reflection of the fundamental importance of the subject area. Heterocyclic chemistry is an underpinning science for a whole host of areas that are vital for mankind’s future.

These include new therapeutic agents, improved molecules to help sustain and enhance food production as well as dyes and electronic molecules that will play an important role in the conservation of energy as well as the next generation of consumer electronics. The meeting will cover many of these areas with presentations from internationally recognized scientists from both industry and academia . Lectures will describe new ways of synthesizing complex new molecules, new mechanistic insights and the issues with the translation of existing and new methodology into industrial settings.

Poster Sessions: There will be two poster sessions at the meeting. Poster presenters will be given preference for acceptance into the meeting. From the poster abstracts received by 1st June 2012, up to four posters will be chosen to be given as "Short Talks" at the meeting. Those interested in showing a poster should submit their abstracts to the Conference Chair.

Social Functions: A wine tasting will be held at Ochre Court on Thursday afternoon between 4:00 pm - 6:00 pm.

Contributors
SUNDAY
2:00 pm - 9:00 pmArrival and Check-in (Office Closed 6:00 pm - 7:00 pm)
6:00 pmDinner
7:30 pm - 7:40 pmWelcome / Introductory Comments by GRC Site Staff
7:40 pm - 9:30 pmNew Strategies for Heterocycle Synthesis I
Discussion Leader: John Wood (Vice Chair,Colorado State University)
7:40 pm - 8:20 pmMark Lautens (University of Toronto)
"No Strain, No Gain? Lessons in Catalysis"
8:20 pm - 8:30 pmDiscussion
8:30 pm - 8:40 pmJared Shaw (University of California, Davis)
"Multicomponent Reactions and Tandem Processes for the Synthesis of Complex Heterocycles"
8:40 pm - 8:45 pmDiscussion
8:45 pm - 9:25 pmErick Carriera (ETH Zurich)
"Surpises and Discovery with Heterocycles"
9:25 pm - 9:30 pmDiscussion
MONDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmCatalysis in Heterocycle Synthesis
Discussion Leader: Hien Nguyen (University of Iowa)
9:00 am - 9:40 amTamejiro Hiyama (Kyoto University)
"Post Cross-Coupling Approach for Conjugated Heterocycles"
9:40 am - 9:50 amDiscussion
9:50 am - 10:20 amGroup Photo / Coffee Break
10:20 am - 11:10 amSherry Chemler (University at Buffalo)
"Copper-catalyzed enantioselective heterocycle synthesis"
11:10 am - 11:20 amDiscussion
11:20 am - 11:40 amDaniel. J. Weix (University of Rochester)
"Nucleophile-Free Cross-Coupling: Mechanism and Scope"
11:40 am - 11:45 amDiscussion
11:45 am - 12:20 pmHuan Wang (Glaxosmithkline)
"Ring Closing Metathesis in the Synthesis of SB462795: Reduction of Catalyst Loading"
12:20 pm - 12:30 pmDiscussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session #1 (Convenor John Wood, Vice Chair)
6:00 pmDinner
7:30 pm - 9:30 pmHeterocyclic Natural Products
Discussion Leader: Sheila Hauck (AstraZeneca)
7:30 pm - 8:10 pmJim Anderson (UCL, UK)
"New Heterocycles using 1,2-Diamines from the Nitro-Mannich Reaction"
8:10 pm - 8:30 pmDiscussion
8:30 pm - 9:10 pmWilliam 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 pmDiscussion
TUESDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmBiological Aspects of Heterocyclic Chemistry
Discussion Leader: Mark Behnke (National Institutes of Health)
9:00 am - 9:35 amShuang Liu (Albany Molecular Research)
"The Discovery of Novel Triple Reuptake Inhibitors"
9:35 am - 9:45 amDiscussion
9:45 am - 10:25 amDennis Dougherty (Caltech)
"The Cation-π Interaction in Chemistry and Biology"
10:25 am - 10:35 am Discussion
10:35 am - 11:05 amCoffee Break
11:05 am - 11:35 amChong 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 pmThomas 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 pmLunch
1:30 pm - 6:00 pmFree Time
6:00 pmDinner
7:30 pm - 9:30 pmNew Strategies for Heterocycle Synthesis
Discussion Leader: Daniel Elbaum (Pfizer)
7:30 pm - 8:10 pmTomislav Rovis (Colorado State University)
"Design and Utility of Chiral Carbenes for Asymmetric Umpolung"
8:10 pm - 8:20 pmDiscussion
8:20 pm - 8:35 pmScott Bagley (Pfizer)
"Synthetic Strategies for Spiro-Heterocyclic ACC Inhibitors"
8:35 pm - 8:40 pmDiscussion
8:40 pm - 9:20 pmArmido Studer (University of Munster, Germany)
"Nitroxides as mild oxidants in synthesis"
9:20 pm - 9:30 pmDiscussion
WEDNESDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmAdvances in the Synthesis of Heterocyclic Compounds
Discussion Leader: Scott Sutton (Pfizer)
9:00 am - 9:40 amTim Gallagher (University of Bristol, UK)
"Exploring Cytisine"
9:40 am - 9:50 amDiscussion
9:50 am - 10:30 amDavid Chen (Seoul National University, South Korea)
"Strategies and Opportunities in the Synthesis of Heterocyclic Natural Products"
10:30 am - 10:40 amDiscussion
10:40 am - 10:50 amBusiness Meeting, Part I
Nominations for the next Vice Chair
10:50 am - 11:10 amCoffee Break
11:10 am - 11:40 amNorito Takenaka (University of Miami)
"Asymmetric Catalysis with Helical-Chiral Pyridines"
11:40 am - 11:45 am Discussion
11:45 am - 12:20 pmYi-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 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session #2 (Convenor John Wood, Vice Chair)
6:00 pmDinner
7:30 pm - 9:30 pmTarget synthesis in Heterocyclic Chemistry
Discussion Leader: Stacey E. Brenner-Moyer (The City University of New York at Brooklyn College)
7:30 pm - 8:10 pmDavid Black (University of New South Wales, Australia)
"Macrocyclic Tetraindolyls: Indorphyrins and related structures as potential new foundation molecules"
8:10 pm - 8:20 pmDiscussion
8:20 pm - 8:35 pmSebastien Caille (Amgen)
"Catalytic Asymmetric Synthesis of a Tertiary Benzylic Carbon Center via Phenol-Directed Alkene Hydrogenation"
8:35 pm - 8:40 pmDiscussion
8:40 pm - 9:20 pmJohn 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 pmDiscussion
THURSDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmMechanisms in Heterocyclic Chemistry
Discussion Leader: Chris Grote (Covidien)
9:00 am - 9:40 amDonna Blackmond (Scripps)
"Mechanistic Studies in Pyrrolidine-Based Organocatalysis"
9:40 am - 9:50 amDiscussion
9:50 am - 10:25 amMatthew L. Maddess (Merck)
"Process Development and Delivery of a Selective Estrogen Receptor Beta Agonist"
10:25 am 10:35 amDiscussion
10:35 am - 11:05 amBusiness Meeting, Part II
Fill out Conference Evaluation Forms; Discuss future Site & Scheduling preferences; Election of the next Vice Chair
11:05 am - 11:35 amCoffee Break
11:35 am - 12:15 pmGuy Lloyd-Jones (University of Bristol UK)
"Amides and Esters"
12:15 pm - 12:25 pmDiscussion
12:30 pmLunch
1:30 pm - 6:00 pmFree Time
6:00 pmDinner
7:30 pm - 9:30 pmNew Reactions in Heterocycle Synthesis
Discussion Leader: Diane Carrera (Genetech)
7:30 pm - 8:10 pmPaul Murray (Cat.Sci)
"General Catalytic Protocols for the synthesis of Complex Drug Molecules"
8:10 pm - 8:30 pmDiscussion
8:30 pm - 9:10 pmDavid MacMillan (Princeton)
"Multi Catalysis in Chemical Synthesis"
9:10 pm - 9:20 pmDiscussion
9:20 pm - 9:30 pmClosing Remarks (Vice Chair)
FRIDAY
7:30 am - 8:30 amBreakfast
9:00 amDeparture
 
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