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Conference Program
 
Heterocyclic Compounds
June 26 - July 1, 2011
Salve Regina University
Newport, RI
Chair:
Richmond Sarpong

Vice Chair:
David C. Lathbury

The Heterocyclic Compounds GRC, which was initiated in 1964, is one of the longest running Gordon Research Conferences. Its longevity reflects the importance of the subject. Heterocyclic Compounds continue to be of interest to industry and academia. Their rich activity in biological systems is important for pharmaceuticals, agricultural products, and natural products. In the pharmaceutical industry, over 75% of the top 200 brand name drugs incorporate heterocyclic motifs in their structures. Additionally, heterocyclic compounds are important components in dye chemistry, organic electronic materials, and as chelating agents.

The 2011 Heterocyclic Compounds Gordon Research Conference will focus on advances in the field. Topics will include: synthesis, new methodology, biologically active heterocycles, catalysis and pharmaceutical agents. The invited speakers include experts in these areas as well as young up-and-coming scientists. The conference will offer many opportunities for formal and informal discussions with fellow conferees. Poster sessions will allow all interested participants to present their own work.


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 Applications of Heterocycles
Discussion Leader: David Lathbury (Albany Molecular Research Inc.)
7:40 pm - 8:00 pm Abigail Doyle (Princeton)
"Strategies and Methods for the Catalytic Functionalization of Heterocycles"
8:00 pm - 8:05 pm Discussion
8:05 pm - 8:30 pm Armen Zakarian (UCSB)
"Strategies for the Synthesis of Maoecrystal V and other /ent/-Kauranoids"
8:30 pm - 8:35 pm Discussion
8:35 pm - 9:20 pm Andrew Myers (Harvard University)
"Research Directed toward the Natural Antiproliferative Agent Cortistatin A leads to a New and Versatile Synthesis of Isoquinolines" [Lecture in Memory of Dr. David Gin]
9:20 pm - 9:30 pm Discussion
MONDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmHeterocycle Formation and Catalytic Functionalizations
Discussion Leader: Ashton Hamme (Jackson State University)
9:00 am - 9:25 am Vy Dong (Toronto)
"A catalytic and enantioselective approach to lactones and lactams"
9:25 am - 9:30 am Discussion
9:30 am - 9:55 am Jacqueline Milne (Amgen)
"Development and Investigation of Pd-catalyzed C-N Bond Formation: Application To the Synthesis of an Active Pharmaceutical Ingredient"
9:55 am - 10:00 am Discussion
10:00 am Coffee Break / Group Photo (10:15 am)
10:25 am - 10:50 am Eric Ferreira (Colorado State)
"Metal-Catalyzed Directed Functionalizations via Heterocycle Formation"
10:55 am - 11:00 am Discussion
11:00 am - 11:30 am Takashi Ooi (Nagoya University)
"Molecular Design and Synthetic Applications of Chiral 1,2,3-Triazolium Salts"
11:30 am - 11:40 am Discussion
11:40 am - 12:20 pm Andrew Degnan (BMS)
"Heterocyclic Compounds for a New Treatment of Depression"
12:20 pm - 12:30 pm Discussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session #1 (Convenor: David Lathbury)
6:00 pmDinner
7:30 pm - 9:30 pmHeterocycles in Natural Product Synthesis I
Discussion Leader: Sarah Reisman (Caltech)
7:30 pm - 7:50 pm Matthias Brewer (University of Vermont)
"Intramolecular cycloadditions as efficient approaches to polycyclic nitrogen heterocycles"
7:50 pm - 7:55 pm Discussion
7:55 pm - 8:25 pm Neil Garg (UCLA)
"Studies toward the Synthesis of Heterocyclic Natural Products"
8:25 pm - 8:35 pm Discussion
8:35 pm - 9:20 pm Brian Stoltz (Caltech)
"Heterocycles as a Driving Force for Discovery in Organic Chemistry"
9:20 pm - 9:30 pm Discussion
TUESDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmMethodology for Heterocyclic Compounds
Discussion Leader: Brian M. Lawrence (Morehouse College)
9:00 am - 9:20 am Taichi Kano (Kyoto)
"Asymmetric α-functionalizations of aldehydes catalyzed by binaphthyl-based secondary amines"
9:30 am - 9:35 am Discussion
9:35 am - 10:05 am Thomas Colacot (JohnsonMatthey)
"Structure Activity Relationship in Pd-Catalyzed Heteroarylation"
10:05 am - 10:10 am Discussion
10:10 am - 10:25 am Poster Presenter 1
10:25 am - 10:30 am Discussion
10:30 am Coffee Break
10:50 am - 11:30 am Mohammad Movassaghi (MIT)
"Complex Alkaloid Total Synthesis"
11:30 am - 11:35 am Discussion
11:35 am - 12:25 pm Jon Ellman (Yale University)
"New Carbon-Carbon Bond Forming Reactions for Heterocycle Synthesis and Elaboration"
12:25 pm - 12:30 pm Discussion
12:30 pmLunch
1:30 pm - 6:00 pmFree Time
6:00 pmDinner
7:30 pm - 9:30 pmHeterocycles in Natural Product Synthesis I
Discussion Leader: Martha Sarpong (GlaxoSmithKline)
7:30 pm - 8:00 pm Mike Kerr (Western Ontario)
"Total synthesis of heterocyclic natural products enabled by the use of donor-acceptor cyclopropanes"
8:00 pm - 8:05 pm Discussion
8:05 pm - 8:35 pm Darren Dixon (Oxford)
"Catalysis and Cascades in Complex Alkaloid Natural Product Synthesis"
8:35 pm - 8:40 pm Discussion
8:40 pm - 9:20 pm John Wood (Colorado State University)
"Recent Efforts in the Synthesis of Oxindole-Containing Natural Products"
9:20 pm - 9:30 pm Discussion
WEDNESDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmHeterocyclic Processes for Biological Applications
Discussion Leader: Javier Sardina (Santiago de Compostela)
9:00 am - 9:20 am Tom Selby (DuPont)
"Pyrimidinone-substituted Methylsulfonylisoxazolines: Potent Herbicidal Inhibitors of Very Long Chain Fatty Acid Biosynthesis"
9:20 am - 9:25 am Discussion
9:25 am - 9:45 am Stefan France (Georgia Tech)
"Diastereoselective Synthesis of Pyrido[1,2-a]indole-based Alkaloids via Indium-Catalyzed Homo-Nazarov Cyclizations"
9:45 am - 9:50 am Discussion
9:50 am - 10:25 amDaniel Fandrick (Boehringer Ingelheim)
"Stereoselective Propargylations with a Propargyl Borolane and application to Heterocyclic Scaffolds"
10:25 am - 10:30 am Discussion
10:30 am - 10:40 amBusiness Meeting: Part 1
Nominations for the next Vice Chair
10:40 am Coffee Break
11:00 am - 11:15 am Poster Presenter 2
11:15 am - 11:20 am Discussion
11:20 am - 11:35 am Poster Presenter 3
11:35 am - 11:45 am Discussion
11:45 am - 12:25 pm Gary Molander (UPenn)
"Organotrifluoroborates in the Service of Heterocyclic Synthesis"
12:25 pm - 12:30 pm Discussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session #2 (Convenor: David Lathbury)
6:00 pmDinner
7:30 pm - 9:30 pmHeterocycles in Chemical Biology
Discussion Leader: Oladapo Bakare (Howard)
7:30 pm - 7:50 pm Herman Sintim (Maryland)
"Bacterial conversation stoppers- new methodologies for constructing next generation anti-infectives"
7:50 pm - 7:55 pm Discussion
7:55 pm - 8:35 pm Margaret Brimble (Auckland)
"Synthesis of bioactive natural products that contain benzannulated spiroketal heterocycles"
8:35 pm - 8:40 pm Discussion
8:40 pm - 9:20 pm Huw Davies (Emory)
"Stereoselective Synthesis of Heterocycles Using Rhodium Carbene Chemistry"
9:20 pm - 9:30 pm Discussion
THURSDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmSynthesis of Biologically Active Heterocycles
Discussion Leader: Jason Herr (AMRI)
9:00 am - 9:30 am Eric A. Voight (Abbott)
"Synthesis of Pharmacologically Differentiated Heterocyclic TRPV1 Antagonists for the Treatment of Chronic Pain"
9:30 am - 9:35 am Discussion
9:35 am - 9:55 am Brian Aquila (Astra Zeneca)
"The chemistry of AZD4877, a kinesin spindle protein inhibitor"
9:55 am - 10:00 am Discussion
10:00 am - 10:25 am Kevin Cole (Eli Lilly)
"A Novel Vanadium-Catalyzed Arylation in Process Development"
10:25 am - 10:30 am Discussion
10:30 am - 10:50 amBusiness Meeting: Part 2
Fill out Conference Evaluation Forms; Discuss future Site & Scheduling preferences; Election of the next Vice Chair
10:50 am - 11:00 am Coffee Break
11:00 am - 11:15 am Poster Presenter 4
11:15 am - 11:20 am Discussion
11:20 am - 12:00 pm Chris Vanderwal (UC Irvine)
"Complex Molecule Synthesis Inspired by the Zincke Ring-Openings of Pyridines"
12:00 pm - 12:05 pm Discussion
12:05 pm - 12:25 pm Tobias Ritter (Harvard)
"Redox Catalysis with Iron and Palladium"
12:25 pm - 12:30 pm Discussion
12:30 pmLunch
1:30 pm - 6:00 pmFree Time / Optional Wine Tasting Social (4:00 pm - 6:00 pm)
6:00 pmDinner
7:30 pm - 9:30 pmExploring Chemical Space: Heterocycles
Discussion Leader: Rebecca Hoye (Macalester College)
7:30 pm - 8:00 pm Daniel Romo (Texas A&M)
"Natural Products as Enduring Forums for Synthetic Strategy and Biological Discovery"
8:00 pm - 8:10 pm Discussion
8:10 pm - 9:05 pm Stuart Schreiber (Harvard)
"Using small-molecule probes to relate the genetic features of human cancers to drug efficacies"
9:05 pm - 9:15 pm Discussion
9:15 pm - 9:30 pmDavid Lathbury (Albany Molecular Research)
Vice Chair's Closing Remarks
FRIDAY
7:30 am - 8:30 amBreakfast
9:00 amDeparture

 
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