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Heterocyclic Compounds
Gordon Research Conference

Heterocycles: Synthetic Targets, Cellular Probes, and Inhibitors

Dates

June 18-23, 2017

Location

Salve Regina University
Newport, RI Site Information

Organizers

Chair:
Daniel Romo

Vice Chair:
Julia M. Clay

Application Deadline

Applications for this meeting must be submitted by May 21, 2017. Please apply early, as some meetings become oversubscribed (full) before this deadline. If the meeting is oversubscribed, it will be stated here. Note: Applications for oversubscribed meetings will only be considered by the Conference Chair if more seats become available due to cancellations.

Meeting Description

The art of chemical synthesis is driven to a great extent by synthetic chemists seeking to find more efficient routes to heterocyclic compounds; molecules at the core of pharmaceutical agents, bioactive natural products, and materials. Heterocyclic chemistry is an enduring field of organic synthesis that continues to provide amazing innovations in chemical synthesis and profoundly impact our society from novel materials (e.g. organic light emitting diodes) to pharmaceutical agents for treatment of human disease and addictions to altering our eating habits.

The 2017 Heterocyclic Compounds GRC will provide an engaging forum for the presentation of cutting-edge chemical synthesis as pertains to heterocycles including novel methods for their synthesis, applications in basic cell biology along with human and animal health. Highlighted topics include organocatalysis, metal-mediated heterocycle synthesis and functionalization, heterocycles as probes for chemical biology, natural product synthesis and food additives. The conference will include a fantastic schedule of domestic and international speakers bolstered by multiple poster sessions detailing the state of the art of heterocyclic chemistry. Set in the beautiful Salve Regina University site close to Newport, RI and with the cliff seawalk just a short walk away, this conference promises to be a memorable one from the standpoint of chemistry, networking, and venue. Please join us for this idea stimulating chemical conference set in a fantastic location where the frontiers of heterocycle synthesis and their use will be discussed.

Contributors

Meeting Program

Sunday
2:00 pm - 9:00 pmArrival and Check-in
6:00 pmDinner
7:30 pm - 7:40 pmWelcome / Introductory Comments by GRC Site Staff
7:40 pm - 9:30 pmNew Methods for the Synthesis of Heterocyclic Compounds
Discussion Leader: John Wood (Baylor University, USA)
7:40 pm - 7:50 pmOpening Remarks
7:50 pm - 8:05 pmShort Talk Selected from Poster Abstracts
8:05 pm - 8:10 pmDiscussion
8:10 pm - 8:35 pmAaron Aponick (University of Florida, USA)
"StackPhos: Using Chiral Heterocycles as Ligands to Make Chiral Amines"
8:35 pm - 8:45 pmDiscussion
8:45 pm - 9:20 pmGregory Fu (California Institute of Technology, USA)
"Metal-Catalyzed Cross-Couplings of Alkyl Electrophiles"
9:20 pm - 9:30 pmDiscussion
Monday
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmCatalysis Towards Heterocyclic Systems
Discussion Leader: Eric Ferreira (University of Georgia, USA)
9:00 am - 9:20 amAndy Mitchell (Illinois State University, USA)
"Oxidopyrylium-Alkene [5+2] Cycloadditions: A Superb Platform for Training Next Generation Scientists"
9:20 am - 9:30 amDiscussion
9:30 am - 9:55 amJunichiro Yamaguchi (Waseda University, Japan)
"Decarbonylative Transformation of Aromatic Esters and Multi-Arylation of Arenes"
9:55 am - 10:05 amDiscussion
10:05 am - 10:35 amCoffee Break
10:35 am - 11:05 amSuzanne Blum (University of California, Irvine, USA)
"Boron-Heteroatom Addition Reactions"
11:05 am - 11:15 amDiscussion
11:15 am - 11:50 amAbigail Doyle (Princeton University, USA)
"New Directions in Ni-Catalyzed Cross Coupling"
11:50 am - 12:00 pmDiscussion
12:00 pm - 12:30 pmPoster Previews
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
3:00 pm - 4:00 pmPower Hour
The GRC Power Hour is an optional informal gathering open to all meeting participants. It is designed to help address the challenges women face in science and support the professional growth of women in our communities by providing an open forum for discussion and mentoring.
Organizers: Abigail Doyle (Princeton University, USA) and Jennifer Roizen (Duke University, USA)
4:00 pm - 6:00 pmPoster Session
6:00 pmDinner
7:30 pm - 9:30 pmSynthesis of Heterocyclic Natural Products
Discussion Leader: Jennifer Roizen (Duke University, USA)
7:30 pm - 7:55 pmCorinna Schindler (University of Michigan, USA)
"Iron(III)-Catalyzed Carbonyl-Olefin Metathesis"
7:55 pm - 8:05 pmDiscussion
8:05 pm - 8:35 pmScott Rychnovsky (University of California, Irvine, USA)
"Recent Studies in Alkaloid Synthesis"
8:35 pm - 8:45 pmDiscussion
8:45 pm - 9:20 pmRichmond Sarpong (University of California, Berkeley, USA)
"Chemical Synthesis of Complex Molecules Featuring Heterocycles"
9:20 pm - 9:30 pmDiscussion
Tuesday
7:30 am - 8:30 amBreakfast
8:30 amGroup Photo
9:00 am - 12:30 pmSynthetic Strategies, Heterocyclic Tools, and Isolation of Heterocyclic Natural Products
Discussion Leader: Doug Frantz (University of Texas at San Antonio, USA)
9:00 am - 9:25 amMingji Dai (Purdue University, USA)
"New Heterocycle Syntheses for Preparation of Natural Products and Medicinally Important Molecules"
9:25 am - 9:35 amDiscussion
9:35 am - 10:00 amDavid Sarlah (University of Illinois at Urbana-Champaign, USA)
"Dearomative Functionalization with Arenophiles"
10:00 am - 10:10 amDiscussion
10:10 am - 10:40 amCoffee Break
10:40 am - 11:00 amShort Talk Selected from Poster Abstracts
11:00 am - 11:10 amDiscussion
11:10 am - 11:35 amBobby O'Brien (Impossible Foods, Inc., USA)
"Discovery and Synthesis of Dipeptoid-Triazine Ligands for Protein Affinity Purification"
11:35 am - 11:45 amDiscussion
11:45 am - 12:20 pmTadeusz Molinski (University of California, San Diego, USA)
"Marine Natural Products. Chemically Diverse Alkaloids from the Ocean"
12:20 pm - 12:30 pmDiscussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session
6:00 pmDinner
7:30 pm - 9:30 pmOptimization of Routes to Biologically Active Heterocycles
Discussion Leader: Ryan Gianatassio (Biogen, USA)
7:30 pm - 7:50 pmHaiming Zhang (Genentech, Inc., USA)
"Process Research and Development of the Commercial Synthesis of BTK Inhibitor GDC-0853"
7:50 pm - 8:00 pmDiscussion
8:00 pm - 8:20 pmJaemoon Lee (Eisai, Inc., USA)
"Chemistry Innovation - The Driver for Process Chemistry Development of the Orexin Receptor Antagonist"
8:20 pm - 8:30 pmDiscussion
8:30 pm - 8:50 pmKaid Harper (AbbVie, USA)
"Flow Chemistry Solutions to Challenging Synthesis Problems"
8:50 pm - 9:00 pmDiscussion
9:00 pm - 9:20 pmJack Brown (Boehringer-Ingelheim, USA)
"Challenges in the Synthesis and Scale-Up of Phosphorous and Sulfur Containing Heterocycles"
9:20 pm - 9:30 pmDiscussion
Wednesday
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmDesign and Synthesis of Biologically Active Heterocyclic Compounds
Discussion Leader: Cynthia Shafer (Novartis Institutes for Biomedical Research, USA)
9:00 am - 9:25 amLarry Burgess (Array BioPharma, USA)
"Development of a Large Scale Process for a p38 Kinase Inhibitor"
9:25 am - 9:35 amDiscussion
9:35 am - 10:00 amJoseph Warmus (Pfizer, USA)
"Functionalizing Heterocycles: Synthesis of β-Heteroaryl-α-Methyl-β-Amino Acids"
10:00 am - 10:10 amDiscussion
10:10 am - 10:40 amCoffee Break
10:40 am - 11:10 amChrista Chrovian (Janssen R&D, USA)
"Preparation of Fused Triazoles via a Single Pot Cycloaddition / Oxy-Cope Rearrangement Enables the Synthesis and Scaling of Novel P2X7 Antagonists"
11:10 am - 11:20 amDiscussion
11:20 am - 11:50 amThomas McGuire (AstraZeneca, USA)
"Chiral Cyclic Sulfamidates and Their Utility in AZ Oncology Drug Discovery Projects"
11:50 am - 12:00 pmDiscussion
12:00 pm - 12:30 pmPoster Previews
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session
6:00 pmDinner
7:00 pm - 7:30 pmBusiness Meeting
Nominations for the Next Vice Chair; Fill in Conference Evaluation Forms; Discuss Future Site and Scheduling Preferences; Election of the Next Vice Chair
7:30 pm - 9:30 pmNew Strategies to Construct Heterocyclic Compounds
Discussion Leader: Angela Puchlopek-Dermenci (Pfizer, Inc., USA)
7:30 pm - 7:55 pmKami Hull (University of Illinois at Urbana-Champaign, USA)
"Transition Metal-Catalyzed Amination Reactions"
7:55 pm - 8:05 pmDiscussion
8:05 pm - 8:35 pmStefan France (Georgia Institute of Technology, USA)
"Formation of Ring-Fused Heterocycles via Strategic Ring-Opening Cyclizations"
8:35 pm - 8:45 pmDiscussion
8:45 pm - 9:20 pmSteven Weinreb (Pennsylvania State University, USA)
"Studies on Synthesis of Indole Alkaloids"
9:20 pm - 9:30 pmDiscussion
Thursday
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmHeterocycles as Probes for Studying Biology and Human Disease
Discussion Leader: Joseph Topczewski (University of Minnesota, USA)
9:00 am - 9:25 amMartin Schnermann (National Cancer Institute, NIH, USA)
"Near-IR Uncaging Chemistry: Discovery and Applications"
9:25 am - 9:35 amDiscussion
9:35 am - 10:00 amMatthew Maddess (Merck & Co., Inc., USA)
"Synthesis Inspires Design: The Importance of Synthetic Innovations in Drug Discovery and Development"
10:00 am - 10:10 amDiscussion
10:10 am - 10:40 amCoffee Break
10:40 am - 10:55 amShort Talk Selected from Poster Abstracts
10:55 am - 11:05 amDiscussion
11:05 am - 11:35 amMark Rizzacasa (University of Melbourne, Australia)
"Silvestrol: The Good, the Bad and the Ugly"
11:35 am - 11:45 amDiscussion
11:45 am - 12:20 pmStephan Sieber (Technical University of Munich, Germany)
"Heterocyclic Tool Compounds for Manipulating Biological Processes"
12:20 pm - 12:30 pmDiscussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session
6:00 pmDinner
7:30 pm - 9:30 pmKeynote Session: An Outlook on Heterocyclic Chemistry
Discussion Leader: Gary Sulikowski (Vanderbilt University, USA)
7:30 pm - 7:50 pmShort Talk Selected from Poster Abstracts
7:50 pm - 8:00 pmDiscussion
8:00 pm - 8:35 pmNicholas Meanwell (Bristol-Myers Squibb, USA)
"Properties and Applications of Heterocycles in Medicinal Chemistry"
8:35 pm - 8:45 pmDiscussion
8:45 pm - 9:20 pmEric Jacobsen (Harvard University, USA)
"Catalyst-Controlled Glycosylation Reactions"
9:20 pm - 9:30 pmDiscussion
Friday
7:30 am - 8:30 amBreakfast
9:00 amDeparture
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