Sunday
2:00 pm - 9:00 pm
Arrival and Check-in
6:00 pm - 7:00 pm
Dinner
7:30 pm - 7:40 pm
Introductory Comments by GRC Site Staff / Welcome from the GRC Chair
7:40 pm - 9:30 pm
Strategic Approaches to the Preparation of Heterocyclic Natural Products
Discussion Leader: Wei Li (University of Toledo, United States)
7:40 pm - 7:45 pm
Opening Remarks
7:45 pm - 8:15 pm
Daniel Gryko (Institute of Organic Chemistry, Polish Academy of Sciences, Poland)
"Pyrrolo[3,2-b]pyrroles - Electron-Rich Functional Heterocycles"
8:15 pm - 8:25 pm
Discussion
8:25 pm - 8:55 pm
James Lanter (Arkuda Therapeutics, United States)
"Functionalized Oxacycles as Progranulin Enhancers"
8:55 pm - 9:05 pm
Discussion
9:05 pm - 9:20 pm
Vincent Lindsay (North Carolina State University, United States)
"Reactivity of Sulfonylcyclopropanols as Precursors of Amide Homoenolates and Fused Heterocycles"
9:20 pm - 9:30 pm
Discussion
Monday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
New Approaches to Heterocyclic Compound Construction
Discussion Leader: Sudeshna Roy (The University of Mississippi, United States)
9:00 am - 9:30 am
Lee Silverberg (Pennsylvania State University, United States)
"Synthesis and Bioactivity of 2,3-Diaryl-1,3-thiaza-4-ones"
9:30 am - 9:40 am
Discussion
9:40 am - 10:10 am
Larry Yet (University of South Alabama, United States)
"Suzuki-Miyaura and Buchwald-Hartwig Reactions Utilizing a Set of Complimentary Imidazopyridine Phosphine Ligands"
10:10 am - 10:20 am
Discussion
10:20 am - 10:50 am
Coffee Break
10:50 am - 11:20 am
Todd Hyster (Cornell University, United States)
"Photoenzymatic Catalysis: Using Light to Reveal New Enzyme Functions"
11:20 am - 11:30 am
Discussion
11:30 am - 12:00 pm
Anita Mattson (Worcester Polytechnic Institute, United States)
"Enantioselective Dearomatization of Heterocyclic Cations"
12:00 pm - 12:10 pm
Discussion
12:10 pm - 12:30 pm
Poster Previews
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
3:00 pm - 4:00 pm
The GRC Power Hour™
The GRC Power Hour™ is designed to address diversity and inclusion in the scientific workplace by providing a safe environment for informal and meaningful conversations amongst colleagues of all career stages. The program supports the professional growth of all members of our communities, including ethnicity, race and/or gender identity by providing an open forum for discussion and mentoring.
Organizers: Catharine Larsen (University of California, Riverside, United States) and Sudeshna Roy (The University of Mississippi, United States)
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Design and Synthesis of Biologically Active Heterocycles
Discussion Leader: Carmela Molinaro (Genentech, United States)
7:30 pm - 8:00 pm
Stephen Greszler (AbbVie, Inc., United States)
"Selective Synthesis and Functionalization of Heterocycles for CFTR, Immunology, and Virology Targets"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
Tanja Gulder (Leipzig University, Germany)
"Hypervalent Iodane Mediated Halogenations: Versatile Tools for the Exploration of Novel Reactivities and Structural Motifs"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Helene Lebel (Universite de Montreal, Canada)
"Amine Diazotisation as a New Heterocycle Alkylation Process"
9:20 pm - 9:30 pm
Discussion
Tuesday
7:30 am - 8:30 am
Breakfast
8:30 am - 9:00 am
Group Photo
9:00 am - 12:30 pm
Paradigm Shifting Synthesis Technologies
Discussion Leader: Kevin Frankowski (University of North Carolina at Chapel Hill, United States)
9:00 am - 9:30 am
Carl Lovely (University of Texas Arlington, United States)
"Applications of New Synthetic Methods for the Total Synthesis of Cyclic Guanidine Natural Products"
9:30 am - 9:40 am
Discussion
9:40 am - 10:10 am
Oliver Kappe (University of Graz, Austria)
"The Use of Flow Technology for the Synthesis of Heterocycles and Pharmaceuticals"
10:10 am - 10:20 am
Discussion
10:20 am - 10:50 am
Coffee Break
10:50 am - 11:20 am
Sophie Rousseaux (University of Toronto, Canada)
"Nickel-Catalyzed Synthesis and Functionalization of Nitrile-Containing Building Blocks"
11:20 am - 11:30 am
Discussion
11:30 am - 12:00 pm
Kevin Moeller (Washington University in St. Louis, United States)
"From Molecules to Molecular Surfaces: Exploiting the Synergy Between Synthesis and Electrochemistry"
12:00 pm - 12:10 pm
Discussion
12:10 pm - 12:30 pm
Poster Previews
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Catalytic Methods for Heterocyclic Compound Preparation and Functionalization
Discussion Leader: Eric Voight (AbbVie, Inc., United States)
7:30 pm - 8:00 pm
Mingji Dai (Purdue University, United States)
"Chemistry Innovation and Biological Discovery through Natural Product Total Synthesis"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
Wei Li (University of Toledo, United States)
"Regiodivergent and Enantioselective Alkene Difunctionalizations for N-Heterocycles Syntheses"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
John Porco (Boston University, United States)
"Unified Synthesis of the Asnovolins and Related Spiromeroterpenoids"
9:20 pm - 9:30 pm
Discussion
Wednesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
New Reaction Strategies for Heterocyclic Compound Design
Discussion Leaders: Jeffrey Gustafson (San Diego State University, United States)
9:00 am - 9:15 am
Ryan Altman (Purdue University, United States)
"A Deoxyfluoroalkylation Strategy for Accessing Highly-Substituted Aryl and Heteroaryl Trifluoromethanes"
9:15 am - 9:20 am
Discussion
9:20 am - 9:35 am
Robert Comito (University of Houston, United States)
"Direct and Selective Amination Methods for the Synthesis of Nitrogen Heterocycle-Containing Compounds"
9:35 am - 9:40 am
Discussion
9:40 am - 10:10 am
Carmela Molinaro (Genentech, United States)
"P450 Catalyzed Transformations"
10:10 am - 10:20 am
Discussion
10:20 am - 10:50 am
Coffee Break
10:50 am - 11:20 am
Thomas Stevenson (FMC Agricultural Solutions, United States)
"Investigating C-H Activation Chemistry of N-Phenyl Azoles: Discovery of a New Class of Herbicides"
11:20 am - 11:30 am
Discussion
11:30 am - 12:00 pm
David Primer (Loxo Oncology at Lilly, United States)
"Development of a Process to CC-90010: Lessons in Ortho-Bromination, Selective Solubility, and Pd Deactivation"
12:00 pm - 12:10 pm
Discussion
12:10 pm - 12:30 pm
Poster Previews
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:00 pm - 7:30 pm
Business 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 pm
Total Synthesis of Heterocyclic Natural Products
Session in memory of Victor Snieckus and Tom Beattie.
Discussion Leader: Matthew Cook (Unaffiliated, United States)
7:30 pm - 8:00 pm
Aaron Aponick (University of Florida, United States)
"Making Chiral Heterocycles Using Chiral Heterocycles"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
Dennis Wright (University of Connecticut, United States)
"Heterocyclic Enzyme Inhibitors Targeting Drug Resistant Pathogens"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Scott Snyder (University of Chicago, United States)
"Strategies and Tactics for the Rapid Synthesis of Molecular Complexity"
9:20 pm - 9:30 pm
Discussion
Thursday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Route Optimization of Heterocyclic Compounds of Pharmaceutical Relevance
Discussion Leader: Daniel Fandrick (Agios Pharmaceuticals Inc., United States)
9:00 am - 9:30 am
Shengquan Duan (Pfizer, Inc., United States)
"Lorlatinib: From Enabling Synthesis to Commercial Route"
9:30 am - 9:40 am
Discussion
9:40 am - 10:10 am
Liang Zhang (Amgen, United States)
"Process Innovation to Enable the Scalable Manufacture of Sotorasib"
10:10 am - 10:20 am
Discussion
10:20 am - 10:50 am
Coffee Break
10:50 am - 11:20 am
Aaron Sather (Merck & Co., Inc., United States)
"Substitution or Synthesis? Approaches to N-(Hetero)Aryl Piperidines"
11:20 am - 11:30 am
Discussion
11:30 am - 11:45 am
Ryan Allen (Emory University, United States)
"Synthetic Design of Pyrrolyl Natural Products"
11:45 am - 11:50 am
Discussion
11:50 am - 12:05 pm
Jeanne Bolliger (Oklahoma State University, United States)
"Mechanistic Investigations into the Formation of Sulfur-Containing Heterocycles by C–H Bond Functionalization"
12:05 pm - 12:10 pm
Discussion
12:10 pm - 12:30 pm
Poster Previews
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Keynote Session: Construction of Complex Molecular Architectures
Discussion Leader: Scott Sutton (Pfizer, United States)
7:30 pm - 8:10 pm
Brian Aquila (Alkermes, Inc., United States)
"Designing Long Acting Injectable Prodrugs of Naltrexone: Sometimes Brick Dust is a Good Thing"
8:10 pm - 8:20 pm
Discussion
8:20 pm - 9:10 pm
Peter Wipf (University of Pittsburgh, United States)
"Total Synthesis of Indole Alkaloids"
9:10 pm - 9:20 pm
Discussion
9:20 pm - 9:30 pm
Closing Remarks
Friday
7:30 am - 8:30 am
Breakfast
9:00 am
Departure