Gordon Research Conferences
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Conference Program
 
Heterocyclic Compounds
June 28 - July 3, 2009
Salve Regina University
Newport, RI

Initiated in 1964, the GRC on Heterocyclic Compounds is one of the longest running Gordon Research Conferences, which reflects the vitality and importance of the subject matter. Heterocyclic compounds account for well over half of all known organic compounds. Many classes of natural products, as well as a large majority of commercially important drugs, agrochemicals, reprographic materials, dyes, etc., contain heterocyclic rings. Hence the synthesis and study of heterocyclic compounds, is a subject of immense importance both for academia and industry. The continued evolution of this field is crucial to achieving efficient, cost-effective solutions to increasingly complex problems in organic synthesis and to accessing unexplored structural space. Through formal research lectures from outstanding scientists, poster sessions and informal discussions, this conference presents an excellent opportunity to any scientist who is interested in gaining knowledge of the most recent advances in this important field.

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 31 May 2009, 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.


Contributors
Abbott Laboratories
Albany Molecular Research Inc.
Amgen, Inc.
AstraZeneca R&D, Boston
AstraZeneca R&D Charnwood
Bristol-Myers Squibb Company
Eastman Kodak Company
Eli Lilly & Co
FoldRx Pharmaceuticals, Inc.
Gilead Sciences
GlaxoSmithKline
Infinity Pharmaceuticals Inc.
Pfizer (GRC Student Fellowships)
Roche Biosciences, Palo Alto
Sanofi-Aventis
Takeda San Diego, Inc.

SUNDAY
2:00 pm - 9:00 pmArrival and Check-in (Office Closed 6:00 pm - 7:00 pm)
5:00 pm - 6:00 pm Welcome Mixer
6:00 pmDinner
7:30 pm - 7:40 pmWelcome / Introductory Comments by GRC Site Staff and Conference Chair, Chris Moody
7:30 pm - 9:30 pm NEW METHODOLOGY IN THE SYNTHESIS OF HETEROCYCLIC COMPOUNDS I
Discussion Leader: J. Ramon Vargas (Eastman Kodak)
7:40 pm - 8:25 pmJeffrey Aubé (University of Kansas)
"Heterocyclic libraries inspired by natural products and peptides"
8:25 pm - 8:35 pm Discussion
8:35 pm - 9:20 pmViresh Rawal (University of Chicago)
"Recent progress on the total synthesis of indole alkaloids"
9:15 pm - 9:30 pm Discussion
MONDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pm CATALYSIS IN HETEROCYCLIC CHEMISTRY
Discussion Leader: Julia M. Clay (Eli Lilly)
9:00 am - 9:50 amGregory C. Fu (Massachusetts Institute of Technology)
"Palladium- and nickel-catalyzed coupling reactions"
9:50 am - 10:00 am Discussion
10:00 am Coffee Break / Group Photo (10:15 am)
10:30 am - 11:00 amJanis Louie (University of Utah)
"Insights into Ni-catalyzed pyridine formation"
11:00 am - 11:10 am Discussion
11:10 am - 11:40 amTom G. Driver (University of Illinois at Chicago)
"Transition metal-catalyzed reactions of azides"
11:40 am - 11:50 am Discussion
11:50 am - 12:20 pmHelena Malinakova (University of Kansas)
"Transition metal-catalyzed multi-component coupling reactions and reaction sequences for the synthesis of medicinally relevant heterocycles"
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: Ramon Vargas)
6:00 pmDinner
7:30 pm - 9:30 pm SYNTHESIS OF HETEROCYCLIC NATURAL PRODUCTS
Discussion Leader: Tom Pettus (UC Santa Barbara)
7:30 pm - 8:00 pmRichmond Sarpong (University of California, Berkeley)
"A unified strategy for the total synthesis of "miscellaneous" Lycopodium alkaloids"
8:00 pm - 8:10 pm Discussion
8:10 pm - 9:10 pmSamuel J. Danishefsky (Columbia University/Sloan Kettering Institute)
"Biologic level molecules through chemical synthesis"
9:10 pm - 9:30 pm Discussion
TUESDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pm NEW ROUTES TO BIOLOGICALLY ACTIVE HETEROCYCLES I
Discussion Leader: Jon Njardarson (Cornell University)
9:00 am - 9:30 amJohn Gilday (AstraZeneca)
"Identification and development of manufacturing routes to the anilinoquinazoline, gefitinib, active ingredient of Iressa®"
9:30 am - 9:35 am Discussion
9:35 am - 10:20 amMercedes Álvarez (IRB, Barcelona)
"Synthesis of polyheterocyclic nitrogen containing marine natural products"
10:20 am - 10:30 am Discussion
10:30 am Coffee Break
11:00 am - 11:30 amKevin W. Gillman (Bristol Myers Squibb)
"Heterocyclic gamma-secretase inhibitors for the treatment of Alzheimer’s disease"
11:30 am - 11:35 am Discussion
11:35 am - 12:20 pmLouis Barriault (University of Ottawa)
"Harvest in the pericyclic reaction garden"
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 pm HETEROCYCLIC NATURAL PRODUCTS AND THEIR BIOSYNTHESIS
Discussion Leader: George Sheppard (Abbott)
7:30 pm - 8:00 pmSarah E. O’Connor (Massachusetts Institute of Technology)
"Metabolic reprograming of alkaloid biosynthesis"
8:00 pm - 8:05 pm Discussion
8:05 pm - 8:25 pmCraig A. Hutton (University of Melbourne)
"Recent progress in the synthesis of cyclic peptide natural products"
8:25 pm - 8:30 pm Discussion
8:30 pm - 9:20 pmRobert M. Williams (Colorado State University)
"Total synthesis as a vehicle for penetrating biomechanistic puzzles: challenges in heterocyclic natural products chemistry"
9:20 pm - 9:30 pm Discussion
WEDNESDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pm NEW STRATEGIES TOWARDS HETEROCYCLIC COMPOUNDS
Discussion Leader: H. Ila (Indian Institute of Technology, Kanpur)
9:00 am - 9:30 amAnna Mapp (University of Michigan)
"Small molecule transcriptional switches"
9:30 am - 9:35 am Discussion
9:35 am - 10:20 amThorsten Bach (Technische Universität, Munich)
"Heterocycles in photochemical and organometallic reactions"
10:20 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
11:10 am - 11:30 am Neil Garg (UCLA)
"Studies in heterocycle synthesis: indoles, indolines, and indolynes"
11:30 am - 11:35 am Discussion
11:35 am - 12:20 pmDonald Craig (Imperial College, London)
"From aziridines to alkaloids: method development and total synthesis"
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: Ramon Vargas)
6:00 pmDinner
7:30 pm - 9:30 pm NEW METHODOLOGY IN THE SYNTHESIS OF HETEROCYCLIC COMPOUNDS II
Discussion Leader: Jennifer Love (University of British Columbia)
7:30 pm - 8:00 pmPaul Vogt (SiGNa)
"Application of stabilized alkali metals in heterocyclic synthesis"
8:00 pm - 8:05 pm Discussion
8:05 pm - 8:25 pm James P. Stambuli (Ohio State University)
"Nickel-catalyzed synthesis of oxazoles via C-S activation"
8:25 pm - 8:30 pm Discussion
8:30 pm - 9:20 pmSam Zard (École Polytechnique, Paris)
"Adventures in radical chemistry: some unusual routes to heterocycles"
9:20 pm - 9:30 pm Discussion
THURSDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pm NEW ROUTES TO BIOLOGICALLY ACTIVE HETEROCYCLES II
Discussion Leader: Dan Elbaum (FoldRx Pharmaceuticals)
9:00 am - 9:25 amBrian Shook (Johnson & Johnson)
"The design and Synthesis of indenopyrimidines as dual adenosine A2a/A1 antagonists for the treatment of Parkinson's disease"
9:25 am - 9:30 am Discussion
9:30 am - 9:55 amR. Jason Herr (Albany Molecular Research Inc)
"Small adventures in total synthesis"
9:55 am - 10:00 am Discussion
10:00 am - 10:30 amBusiness Meeting Part 2
(Fill out Conference Evaluation Forms; Discuss future Site & Scheduling preferences; Election of the next Vice Chair)
10:30 am Coffee Break
11:00 am - 11:30 amTehshik P. Yoon (University of Wisconsin, Madison)
"Cycloadditions by visible light photocatalysis"
11:30 am - 11:35 am Discussion
11:35 am - 11:55 amAmy Dounay (Pfizer Global R&D)
"Design, synthesis, and pharmacological evaluation of phenoxy pyridyl derivatives as norepinephrine reuptake inhibitors and 5-HT1A partial agonists"
11:55 am - 12:00 pm Discussion
12:00 pm - 12:25 pmScott Coffey (Eli Lilly)
"Process development of an NK-1 antagonist"
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 pm PERSPECTIVES ON HETEROCYCLIC CHEMISTRY
The challenges posed by the synthesis of complex heterocyclic compounds
Discussion Leader: Chris Moody (University of Nottingham)
7:30 am - 8:15 pmJon Rainier (University of Utah)
"Approaches to heterocycles at 4700 feet above sea level"
8:15 pm - 8:20 pm Discussion
8:20 pm - 9:05 pmStephen F. Martin (University of Texas, Austin)
"Recent advances in the synthesis of complex heterocyclic natural products"
9:05 pm - 9:15 pm Discussion
9:15 pm - 9:30 pmJ. Ramon Vargas (Eastman Kodak)
"Vice Chair’s Closing Remarks"
FRIDAY
7:30 am - 8:30 amBreakfast
9:00 amDeparture

 
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