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 Staff / Welcome and Introduction from the Chairs
7:40 pm - 9:30 pm
Creative Approaches to Heterocyclic Targets
Discussion Leader: Florence Williams (University of Iowa, United States)
7:40 pm - 7:45 pm
Opening Remarks
7:45 pm - 8:15 pm
Lisa Marcaurelle (GSK, United States)
"Identification of Molecular Glues by DNA-Encoded Library Technology"
8:15 pm - 8:25 pm
Discussion
8:25 pm - 8:40 pm
Steven Castle (Brigham Young University, United States)
"Microwave-Promoted Iminyl Radical Cyclizations: Application to the Total Synthesis of Virosinine A"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Francisco Gonzalez-Bobes (BMS, United States)
"Adventures in the Development of Complex Pharmaceuticals"
9:20 pm - 9:30 pm
Discussion
Monday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Heterocycles to Probe Biological Activity
Discussion Leader: Jeanne Bolliger (Oklahoma State University, United States)
9:00 am - 9:30 am
Ying Wang (AbbVie, United States)
"Access and Synthesis of Heterocycle Moieties for Efficient Medicinal Chemistry SAR Studies"
9:30 am - 9:40 am
Discussion
9:40 am - 10:10 am
Maryll Geherty (Bristol Myers Squibb, United States)
"Development and Multi-Kilogram Manufacture of Iberdomide (CC-220)"
10:10 am - 10:20 am
Discussion
10:20 am - 10:50 am
Coffee Break
10:50 am - 11:20 am
Dani Schultz (Merck, United States)
"Taming the Unnatural – Advances in Non-canonical Amino Acid Synthesis for Drug Discovery and Beyond"
11:20 am - 11:30 am
Discussion
11:30 am - 12:00 pm
Andrew Parsons (Amgen, Inc., United States)
"Development of a Commercial Manufacturing Process for Sotorasib (AMG 510), a First-in-Class KRASG12C Inhibitor"
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: Florence Williams (University of Iowa, United States) and Stefan France (Georgia Institute of Technology, United States)
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Advances in Catalytic Methods and Mechanisms
Discussion Leader: Zarko Boskovic (University of Kansas, United States)
7:30 pm - 8:00 pm
Helma Wennemers (ETH Zurich, Switzerland)
"Asymmetric Catalysis with Peptides"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
Travis Williams (University of Southern California, United States)
"The Metal Matters: Multi-Metallic Catalysts to Access New Applications of Hydrogen Borrowing Amination"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Andrew McNally (Colorado State University, United States)
"Selective Functionalization of Pyridines, Diazines and Pharmaceuticals via Unconventional Intermediates"
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
Exploring Heterocyclic Chemistry
Discussion Leader: Bérénice Lewandowksi (Vertex Pharmaceuticals, United States)
9:00 am - 9:30 am
Jeffrey Aubé (University of North Carolina at Chapel Hill, United States)
"Collaborative Medicinal Chemistry in Infectious Disease and Neuroscience"
9:30 am - 9:40 am
Discussion
9:40 am - 10:10 am
Courtney Roberts (University of Minnesota, United States)
"Synthesis of Heterocycles Through Aryne Intermediates"
10:10 am - 10:20 am
Discussion
10:20 am - 10:45 am
Coffee Break
10:45 am - 11:00 am
Michaella Caporello (Snapdragon Chemistry, United States)
"Chemistry Problem Solving through Continuous Reactor Design"
11:00 am - 11:10 am
Discussion
11:10 am - 11:40 am
Mary Watson (University of Delaware, United States)
"Deaminative Cross-Couplings"
11:40 am - 11:50 am
Discussion
11:50 am - 12:20 pm
Mark Levin (University of Chicago, United States)
"Single Atom Logic for Skeletal Editing"
12:20 pm - 12:30 pm
Discussion
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
Heterocyclic Natural Products
Discussion Leader: Kevin Kou (UC Riverside, United States)
7:30 pm - 8:00 pm
Jon Njardarson (University of Arizona, United States)
"Heterocycle Inspired Anionic Cascade Adventures"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
Victoria Piunova (Loliware, United States)
"Blue Plastic: Seaweed-Derived Biomass to Replace Single-Use Plastics"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Tadeusz Molinski (University of California, San Diego, United States)
"The 'Endless Sea'. Discovery of Unexpected New Molecules from the Sand Beneath Your Feet"
9:20 pm - 9:30 pm
Discussion
Wednesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Novel Strategies of Construction with Heterocycles
Discussion Leader: Cheyenne Brindle (Trinity College, United States)
9:00 am - 9:30 am
Donald Watson (Univesity of Delaware, United States)
"Heterocycle Preparation Using aza-Heck Reactions"
9:30 am - 9:40 am
Discussion
9:40 am - 10:10 am
Sidney Wilkerson-Hill (The University of North Carolina at Chapel Hill, United States)
"Incorporation of Orphaned Cyclopropanes in Heterocyclic Molecules"
10:10 am - 10:20 am
Discussion
10:20 am - 10:50 am
Coffee Break
10:50 am - 11:20 am
Emily Wearing (University of Michigan, United States)
"New Transformations for the Synthesis of Azetidines and Oxetanes"
11:20 am - 11:30 am
Discussion
11:30 am - 12:00 pm
Marvin Parasram (New York University, United States)
"Anaerobic Oxygen Atom Transfer Reactions Promoted by Photoexcited Nitroarenes"
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
Harnessing Heterocyclic Compounds as Therapeutics
Discussion Leader: Dave Martin (University of Iowa, United States)
7:30 pm - 8:00 pm
Vanessa Marx (Novartis Institutes for Biomedical Research, United States)
"Discovery of a Novel Quinoline-Based Proteasome Inhibitor for Human African Trypanosomiasis (HAT)"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
Charles Yeung (Merck & Co., Inc., United States)
"Disrupting How We Make Molecules: Molecular Editing and 3D Rich Architectures"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Sabine Hadida (Vertex Pharmaceuticals, United States)
"Discovery of CFTR Modulators for The Treatment of Cystic Fibrosis"
9:20 pm - 9:30 pm
Discussion
Thursday
7:30 am - 8:30 am
Breakfast
8:30 am - 9:00 am
Business Meeting
Nominations for the Next Vice Chair(s); Complete the GRC Evaluation Forms; Discuss Future Dates and Venue; Election of the Next Vice Chair(s)
9:00 am - 12:30 pm
Transforming Heterocycles
Discussion Leader: Myles Smith (UT Southwestern Medical Center, United States)
9:00 am - 9:30 am
Thomas Beauchamp (Eli Lilly and Company, United States)
"Adventures in Early Process Development from the Lilly Portfolio"
9:30 am - 9:40 am
Discussion
9:40 am - 10:10 am
Ryan Altman (Purdue University, United States)
"Accessing Fluoroalkyl Heterocycles by Deoxyfluoroalkylation and Reactions of Fluorinated Alkenes"
10:10 am - 10:20 am
Discussion
10:20 am - 10:45 am
Coffee Break
10:45 am - 11:00 am
Benoit Cardinal-David (AbbVie, United States)
"Evolution of ABBV-105 Synthetic Route and Process Development to Phase 2"
11:00 am - 11:10 am
Discussion
11:10 am - 11:40 am
Lauren Sirois (Genentech, Inc., United States)
"Rapid Evolution of the Manufacturing Process for KRAS Inhibitor GDC-6036"
11:40 am - 11:50 am
Discussion
11:50 am - 12:20 pm
Joyann Donaldson (Pfizer, United States)
"Synthesis of Medicinally Relevant Isoquinolones and Derivatives Thereof via Rh-Catalyzed C-H Activation"
12:20 pm - 12:30 pm
Discussion
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: Innovations Fueled by Heterocycles
Discussion Leader: Stefan France (Georgia Institute of Technology, United States)
7:30 pm - 7:45 pm
Naoko Ichiishi (Sanofi, United States)
"Improvement on the Synthesis and Thermostability of Imidates Showcased from Drug Discovery to Materials Science"
7:45 pm - 7:55 pm
Discussion
7:55 pm - 8:30 pm
Alison Wendlandt (Massachusetts Institute of Technology, United States)
"Selective Interconversion of Carbohydrate Isomers"
8:30 pm - 8:40 pm
Discussion
8:40 pm - 9:15 pm
Dean Toste (University of California, United States)
"Synthesis and Application of Heterocycles in Selectivity-Driven Chemistry"
9:15 pm - 9:25 pm
Discussion
9:25 pm - 9:30 pm
Closing Remarks
Friday
7:30 am - 8:30 am
Breakfast
9:00 am
Departure