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Conference Program
 
Heterocyclic Compounds
June 16-21, 2013
Salve Regina University
Newport, RI
Chair:
John L. Wood

Vice Chair:
George S. Sheppard

The Gordon Research Conference on Heterocyclic Compounds has a long standing tradition of bringing together chemists from academics and industry to discuss recent advances in the synthesis, methods, isolation and biology of molecules possessing diverse arrays of heterocycles. Importantly, the latter can be found in the majority of marketed pharmaceutical agents, agricultural products, and materials.

The 2013 conference will feature numerous speakers from both the academic and industrial sectors who will present lectures on topics ranging from synthetic method development and heterocyclic natural products total synthesis to the chemistry and biology of novel antibody recruiting molecules, green chemistry and both process and medicinal chemistry research. In contrast to many previous conferences, nearly half of the scheduled speakers from academics are young pre-tenure scientists whose research programs have already been internationally recognized. As always, the conference will be organized to allow many opportunities for informal discussion outside the scheduled lectures and will include two poster sessions. In addition, four speakers will be selected from the pool of submitted posters to present "Short Talks" on their research.

Celebration of Professor E.C. Taylor and his Contributions to Heterocyclic Chemistry: Many who have regularly attended the Heterocyclic Compounds GRC or, for that matter, been engaged in heterocyclic chemistry research, will be well aware of Professor Taylor’s contributions to the field. In honor of his 90th birth year and many contributions to our field the Thursday lectures and afternoon wine tasting will be dedicated to Professor Taylor and his many co-workers. In addition, the meeting will close Thursday evening with a retrospective lecture by Professor Taylor.


Contributors

SUNDAY
4:00 pm - 8:00 pmArrival and Check-in
6:00 pmDinner
7:30 pm - 7:40 pmWelcome / Introductory Comments by GRC Site Staff
7:40 pm - 9:30 pmHeterocyclic Compounds in Natural Products Synthesis I
Discussion Leader: R. Nancy Tao (Yale University)
7:40 pm - 8:25 pmGlenn C. Micalizio (Scripps Research Institute)
"Metallacycle-Mediated Alkene-Imine Cross-Coupling in Heterocycle Synthesis"
8:25 pm - 8:35 pmDiscussion
8:35 pm - 9:20 pmAmos B. Smith, III (The University of Pennsylvania)
"Evolution of Anion Relay Chemistry (ARC) Leading to Siloxane-Based Transfer Agents for Palladuim Cross-Coupling Reactions"
9:20 pm - 9:30 pmDiscussion
MONDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmHeterocyclic Compounds of Pharmaceutical Relevance
Discussion Leader: Tatsuya Shirahata (Kitasato University)
9:00 am - 9:35 amBrian Lucas (Amgen)
"A Facile Approach to the Piperidinone Class of MDM2/p53 Inhibitors"
9:35 am - 9:45 amDiscussion
9:45 am - 10:20 amPrabhakar Jadhav (Eli Lilly)
"Discovery of Potent, Orally Bioavailable, Nonpetide Cathepsin S Inhibitor Lacking Interactions with Catalytic Cysteine"
10:20 am - 10:30 amDiscussion
10:30 amGroup Photo / Coffee Break
11:00 am - 11:35 amDon Pinto (Bristol-Myers Squibb)
"Next Generation Antithrombotics; Lessons Learned in Discovering a Drug"
11:35 am - 11:45 amDiscussion
11:45 am - 12:20 pmJohn Maxwell (Vertex)
"Use of Heterocycles in Drug Discovery"
12:20 pm - 12:30 pmDiscussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session I
6:00 pmDinner
7:30 pm - 9:30 pmMethods for the Synthesis of Heterocyclic Compounds I
Discussion Leader: Graham C. Murphy (University of Waterloo)
7:30 pm - 8:10 pmVictor Snieckus (Queen's University)
"Progress in Aromatic Metalation with a Tribute to Ted Taylor"
8:10 pm - 8:20 pmDiscussion
8:20 pm - 8:35 pmAnita Mattson (The Ohio State University)
8:35 pm - 8:40 pmDiscussion
8:40 pm - 9:20 pmKarl Hale (Queen's University, Belfast)
"Total Synthesis Studies on Pyran-Containing Antitumor Natural Products"
9:20 pm - 9:30 pmDiscussion
TUESDAY
Important Note: Please be aware that the order of events on Tuesday, June 18 deviates from the standard schedule that is used on all other days of the meeting. The revised schedule is displayed below.
7:30 am - 8:30 amBreakfast
8:30 am - 10:30 amFree Time
10:30 am - 12:30 pmPoster Session I
12:30 pmLunch
1:30 pm - 5:00 pmMethods for the Synthesis of Heterocyclic Compounds II
Discussion Leader: Jenny L. Roizen (Duke University)
1:30 pm - 2:05 pmJavier Read de Alaniz (University of California, Santa Barbara)
"Methods for Carbon-Nitrogen Bond Formation"
2:05 pm - 2:15 pmDiscussion
2:15 pm - 2:55 pmRyan Looper (University of Utah)
"Propargylguanidine hydroaminations and their applications to important heterocyclic systems"
2:55 pm - 3:05 pmDiscussion
3:05 pmCoffee Break
3:20 pm - 4:00 pmJón Njardarson (University of Arizona)
"New Heterocyclic Sagas from the Sonoran Desert"
4:00 pm - 4:10 pmDiscussion
4:10 pm - 4:50 pmSeth Herzon (Yale University)
"Target-Driven Total Synthesis"
4:50 pm - 5:00 pmDiscussion
5:00 pm - 6:00 pmFree Time
6:00 pmDinner
7:30 pm - 9:30 pmCatalytic Methods for the Synthesis of Heterocyclic Compounds
Discussion Leader: Neil Garg (University of California, Los Angeles)
7:30 pm - 8:10 pmLiz Jarvo (University of California, Irvine)
"Mechanism-Based Design and Development of Nickel-Catalyzed Stereospecific Cross-Coupling Reactions"
8:10 pm - 8:20 pmDiscussion
8:20 pm - 8:35 pmDavid Lupton (Monash University)
8:35 pm - 8:40 pmDiscussion
8:40 pm - 9:20 pmJoe Ready (University of Texas, Southwest Medical Center)
"Synthesis of small molecules with anti-cancer properties"
9:20 pm - 9:30 pmDiscussion
WEDNESDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmHeterocyclic Compounds in Natural Products Synthesis II
Discussion Leader: Frances R. Blase (Haverford University)
9:00 am - 9:45 amToshiaki Sunazuka (Kitastato Institute)
"Total synthesis of novel polycyclic bioactive indole alkaloids"
9:45 am - 9:55 amDiscussion
9:55 am - 10:10 amGuangbin Dong (University of Texas, Austin)
10:10 am - 10:15 amDiscussion
10:15 amCoffee Break
10:40 am - 11:25 amCarol Taylor (Louisiana State University)
"Running Rings Around Peptides"
11:25 am - 11:35 amDiscussion
11:35 am - 12:20 pmGary Sulikowski (Vanderbilt Universiyt)
"Synthesis and Study of Heterocyclic Natural Products"
12:20 pm - 12:30 pmDiscussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session II
7:30 pm - 9:30 pmBiological Applications of Heterocyclic Compounds
Discussion Leader: Eric M. Ferreira (Colorado State University)
7:30 pm - 8:10 pmGeorge Moniz (Eisai)
"Process Research and Development Towards Medicinally Relevant Heterocyclic Compounds"
8:10 pm - 8:20 pmDiscussion
8:20 pm - 8:35 pmDaniel Fandrick (Boehringer-Ingelheim)
8:35 pm - 8:40 pmDiscussion
8:40 pm - 9:20 pmDavid Spiegel (Yale University)
"Synthetic and Biological Studies of Advanced Glycation End-Products"
9:20 pm - 9:30 pmDiscussion
THURSDAY
7:30 am - 8:30 amBreakfast
8:30 am - 9:00 amBusiness Meeting
Nominations for the next Vice Chair; Fill out Conference Evaluation Forms; Discuss future Site & Scheduling preferences; Election of the next Vice Chair
9:00 am - 12:30 pmThe Evolution of a Research Program in Heterocyclic Chemistry
Discussion Leader: Brian E. Love (East Carolina University)
9:00 am - 9:35 amJohn Macor (Bristol-Myers Squibb)
"Heterocycles as Bioisosteres in the Discovery of Orally Active CGRP Receptor Antagonists for the Treatment of Migraine"
9:35 am - 9:45 amDiscussion
9:45 am - 10:20 amHuw M. L. Davies (Emory University)
"Unusual Reactions Between Rhodium Carbenes and Heterocycles"
10:20 am - 10:30 amDiscussion
10:30 amCoffee Break
11:00 am - 11:35 amJohn Warner (Warner-Babcock Institute)
"Heterocycles in Materials Science"
11:35 am - 11:45 amDiscussion
11:45 am - 12:20 pmStephen F. Martin (University of Texas, Austin)
"Total Synthesis of Heterocyclic Natural Products"
12:20 pm - 12:30 pmDiscussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session II
7:30 pm - 9:30 pmA Perspective on Heterocyclic Compounds in Academics and Industry
Discussion Leader: John LaMattina (PureTech Ventures)
7:30 pm - 7:50 pmLouis Jungheim (Roosevelt University and LNJ Consulting)
"Pyrazolidinones and oxazoles, two of my favorite heterocycles"
7:50 pm - 8:00 pmDiscussion
8:00 pm - 8:20 pmPaul Reider (Princeton University)
"The Synthesis of Heterocycles as Novel Agents in the Fight Against TB, Malaria and Other Neglected Diseases"
8:20 pm - 8:30 pmDiscussion
8:30 pm - 9:20 pmE. C. Taylor (Princeton University)
"Reflections on 67 Years of Heterocyclic Chemistry"
9:20 pm - 9:30 pmDiscussion
FRIDAY
7:30 am - 8:30 amBreakfast
9:00 amDeparture

 
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