Sunday |
2:00 pm - 9:00 pm | Arrival and Check-in |
6:00 pm | Dinner |
7:30 pm - 7:40 pm | Welcome / Introductory Comments by GRC Site Staff |
7:40 pm - 9:30 pm | Strategies
for Preparing Complex Molecules |
| Discussion Leader: Scott Sieburth (Temple University, USA) |
7:40 pm - 8:05 pm | Kevin Brown (Indiana University, USA) "No Strain, No Gain: Advances in the Synthesis and Use of Cyclobutanes" |
8:05 pm - 8:15 pm | Discussion |
8:15 pm - 8:40 pm | David Waller (Merck & Co. Inc., USA) "The Cross-Coupling Approach to Cephalosporin Antibiotics" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Andre Beauchemin (University of Ottawa, Canada) "Reaction Development Using Temporary Intramolecularity and Amphoteric Isocyanates" |
9:20 pm - 9:30 pm | Discussion |
Monday |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Inspired
by Nature: Biomimetic Syntheses,
Biocatalysis, and Applications of "Large Molecules" |
| Discussion Leaders: Hosea Nelson (University of California, Los Angeles, USA) and Pamela Tadross (Merck & Co. Inc., USA) |
9:00 am - 9:30 am | Thomas Maimone (University of California, Berkeley, USA) "Synthesis of Complex Terpenes from Simple Precursors" |
9:30 am - 9:45 am | Discussion |
9:45 am - 10:15 am | Jared Lewis (University of Chicago, USA) "Engineering Proteins for Selective Catalysis" |
10:15 am - 10:30 am | Discussion |
10:30 am - 11:00 am | Coffee Break |
11:00 am - 11:30 am | Robert Linhardt (Rensselaer Polytechnic Institute, USA) "Chemoenzymatic Synthesis of Heparin and Low Molecular Weight Heparins" |
11:30 am - 11:45 am | Discussion |
11:45 am - 12:15 pm | David Entwistle (Codexis Inc., USA) "Enzyme Evolution for Pharmaceutical Manufacture" |
12:15 pm - 12:30 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 4:00 pm | Free Time |
4:00 pm - 6:00 pm | Poster Session |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Going
with or Against the Flow: Guidelines and Applications for Continuous-Flow
Operations |
| Discussion Leader: Dominique Hebrault (Mettler Toledo, USA) |
7:30 pm - 8:00 pm | Nicola Pohl (Indiana University, USA) "A Systems Approach to Tackling the Challenges of Carbohydrate Synthesis and Analysis" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Klavs Jensen (Massachusetts Institute of Technology, USA) "Automated Organic Chemistry for Screening, Optimization, and Scaling" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Martin Johnson (Eli Lilly and Company, USA) "Applications of Continuous Reactors in Pharmaceutical Manufacturing" |
9:20 pm - 9:30 pm | Discussion |
Tuesday |
7:30 am - 8:30 am | Breakfast |
8:30 am | Group Photo |
9:00 am - 12:30 pm | Precious
or Non-Precious Metals: Organometallic
Reagents Using or Avoiding Transition Metals, Precious Metals, and Rare Earth
Elements |
| Discussion Leaders: Jennifer Roizen (Duke University, USA) and Vladimir Gevorgyan (University of Illinois at Chicago, USA) |
9:00 am - 9:30 am | Olafs Daugulis (University of Houston, USA) "New Methods for Carbon-Hydrogen Bond Functionalization" |
9:30 am - 9:45 am | Discussion |
9:45 am - 10:15 am | Donald Watson (Univesity of Delaware, USA) "Recent Progress in Heteroatomic Heck Reactions" |
10:15 am - 10:30 am | Discussion |
10:30 am - 11:00 am | Coffee Break |
11:00 am - 11:30 am | Kami Hull (University of Illinois at Urbana-Champaign, USA) "Transition Metal-Catalyzed Amination and Amidation Reactions" |
11:30 am - 11:45 am | Discussion |
11:45 am - 12:15 pm | Veronique Gouverneur (Oxford University, United Kingdom) "Fluorine Chemistry: Chemical, Radiochemical and Clinical Advances" |
12:15 pm - 12:30 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 4:00 pm | Free Time |
4:00 pm - 6:00 pm | Poster Session |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | From Flask to Reactor:
Strategies and Tactics for Scale-Up |
| Discussion Leader: Sergey Pronin (University of California, Irvine, USA) |
7:30 pm - 8:00 pm | Brenda Burke (Gilead Sciences, Inc., USA) "Process Chemistry Development of Ledipasvir - NS5A Inhibitor in HarvoniĀ® for Hepatitis C Treatment" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Michael Bech Sommer (Awapatent A/S, Denmark) "Courtroom Chemistry and Molecules with a Legal Twist" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Ryan Shenvi (Scripps Research Institute, USA) "Persistence" |
9:20 pm - 9:30 pm | Discussion |
Wednesday |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Enlightening Tools: Photoredox Catalysis and
Other "One-Electron" Chemistry |
| Discussion Leaders: David Michaelis (Brigham Young University, USA) and Daniele Leonori (The University of Manchester, United Kingdom) |
9:00 am - 9:30 am | Melanie Sanford (University of Michigan, USA) "Recent Developments in Catalytic C-H Functionalization" |
9:30 am - 9:45 am | Discussion |
9:45 am - 10:15 am | Tehshik Yoon (University of Wisconsin-Madison, USA) "A General Strategy for Stereocontrol in Photochemical Reactions" |
10:15 am - 10:30 am | Discussion |
10:30 am - 11:00 am | Coffee Break |
11:00 am - 11:30 am | Robert Knowles (Princeton University, USA) "Proton Coupled Electron Transfer in Organic Synthesis" |
11:30 am - 11:45 am | Discussion |
11:45 am - 12:15 pm | David MacMillan (Princeton University, USA) "The Use of Photoredox Catalysis to Invent or Discover Unique One-Electron Mediated Reactions" |
12:15 pm - 12:30 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 4:00 pm | Free Time |
4:00 pm - 6:00 pm | Poster Session |
6:00 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 | Approaches for Innovative Medicines |
| Discussion Leader: Yi-Yin Ku (AbbVie, USA) |
7:30 pm - 8:00 pm | Nicole Goodwin (GlaxoSmithKline, USA) "Split Kinase Personalities: Type I and Type III Inhibitors of LIMK2" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Thomas Razler (Bristol-Myers Squibb, USA) "Development of the Commercial Synthesis of Gamma Secretase Inhibitor BMS-708163 (Avagacestat)" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Kris Jones (Pfizer, USA) "Development of Ertugliflozin, a Novel SGLT2i Inhibitor: From Sugar to Co-Crystal" |
9:20 pm - 9:30 pm | Discussion |
Thursday |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Advances in Catalysis and Reaction Mechanisms |
| Discussion Leaders: Silas Cook (Indiana University, USA) and Matthew Beaver (Amgen, USA) |
9:00 am - 9:30 am | Matthew Meyer (University of California, Merced, USA) "Exploring the Selectivity Problem in Chemistry Using Isotopes" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Jean-Philip Lumb (McGill University, Canada) "Driving Synthesis by Oxidation" |
10:10 am - 10:20 am | Discussion |
10:20 am - 10:35 am | Coffee Break |
10:35 am - 11:00 am | Johan Wennerberg (Chemoswed AB, Sweden) "Development of a Practical and Safe Synthesis of ABR-215062" |
11:00 am - 11:10 am | Discussion |
11:10 am - 11:35 am | John Limanto (Merck Sharp & Dohme, USA) "Development of a Long-Term Manufacturing Route to an HCV NS5b Inhibitor" |
11:35 am - 11:45 am | Discussion |
11:45 am - 11:55 am | Jill Caputo (University of Rochester, USA) "Teaching an Old Dot New Tricks: The Use of Quantum Dots in Photoredox Catalysis" |
11:55 am - 12:00 pm | Discussion |
12:00 pm - 12:10 pm | Justin Mohr (University of Illinois at Chicago, USA) "Regio- and Stereocontrol with Anions and Radicals" |
12:10 pm - 12:15 pm | Discussion |
12:15 pm - 12:25 pm | Alexandr Shafir (Institute of Chemical Research of Catalonia (ICIQ), Spain) "New Concepts for Engaging the Haloarenes in CH Functionalization: Halogen Retention for Downstream Diversification" |
12:25 pm - 12:30 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 4:00 pm | Free Time |
4:00 pm - 6:00 pm | Poster Session |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Keynote Session: The Mystery of Organic Chemistry: Exploiting Surprises, Molecular Machines,
and Legerdemain |
| Discussion Leader: Travis Remarchuk (Denali Therapeutics, Inc., USA) |
7:30 pm - 8:00 pm | Sergey Pronin (University of California, Irvine, USA) "New Methods and Strategies for the Synthesis of Indole Diterpenes" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Bo Qu (Boehringer Ingelheim Pharmaceuticals, USA) "An Ideal Enantioselective Synthesis for BI 11β-HSD Inhibitor" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Steven Raw (AstraZeneca, United Kingdom) "Osimertinib Mesylate: Process Development and Scale-Up of an API on the Critical Path" |
9:20 pm - 9:30 pm | Discussion |
Friday |
7:30 am - 8:30 am | Breakfast |
9:00 am | Departure |