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Organic Reactions & Processes
Gordon Research Conference

Emerging Concepts and Technologies for Organic Processes

Dates

July 17-22, 2016

Location

Stonehill College
Easton, MA

Organizers

Chairs:
Neal G. Anderson & Vy Dong

Vice Chairs:
Silas Cook & Travis P. Remarchuk

Meeting Description

The 2016 GRC meeting in Organic Reactions and Processes will bring together researchers from across academic and industrial labs, who are engaged in the art and science of making molecules. This meeting will balance our thirst for the fundamental with our need for the practical. Invited lectures will feature researchers who are developing new ways to activate common functional groups and devise creative strategies to complex molecules. While in the early stages of development, these ideas will ultimately result in valuable tools for organic synthesis. Process chemists in industry have also been invited to present their applications of current technologies for the large-scale synthesis of medicinally relevant targets. A broad range of topics has been selected to inform and inspire participants in areas that may be new to them, and there will be many opportunities for discussions. Some of the participants' posters will be highlighted as short presentations. Attendees will thus get many chances to see emerging concepts and robust technologies applied in an innovative fashion. On the last night of the conference, we will be reminded of the magic of chemistry in our everyday lives.

Contributors

Final 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 pmStrategies for Preparing Complex Molecules
Discussion Leader: Scott Sieburth (Temple University, USA)
7:40 pm - 8:05 pmKevin Brown (Indiana University, USA)
"No Strain, No Gain: Advances in the Synthesis and Use of Cyclobutanes"
8:05 pm - 8:15 pmDiscussion
8:15 pm - 8:40 pmDavid Waller (Merck & Co. Inc., USA)
"The Cross-Coupling Approach to Cephalosporin Antibiotics"
8:40 pm - 8:50 pmDiscussion
8:50 pm - 9:20 pmAndre Beauchemin (University of Ottawa, Canada)
"Reaction Development Using Temporary Intramolecularity and Amphoteric Isocyanates"
9:20 pm - 9:30 pmDiscussion
Monday
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmInspired 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 amThomas Maimone (University of California, Berkeley, USA)
"Synthesis of Complex Terpenes from Simple Precursors"
9:30 am - 9:45 amDiscussion
9:45 am - 10:15 amJared Lewis (University of Chicago, USA)
"Engineering Proteins for Selective Catalysis"
10:15 am - 10:30 amDiscussion
10:30 am - 11:00 amCoffee Break
11:00 am - 11:30 amRobert Linhardt (Rensselaer Polytechnic Institute, USA)
"Chemoenzymatic Synthesis of Heparin and Low Molecular Weight Heparins"
11:30 am - 11:45 amDiscussion
11:45 am - 12:15 pmDavid Entwistle (Codexis Inc., USA)
"Enzyme Evolution for Pharmaceutical Manufacture"
12:15 pm - 12:30 pmDiscussion
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.
Organizer: Pamela Tadross (Merck & Co. Inc., USA)
4:00 pm - 6:00 pmPoster Session
6:00 pmDinner
7:30 pm - 9:30 pmGoing with or Against the Flow: Guidelines and Applications for Continuous-Flow Operations
Discussion Leader: Dominique Hebrault (Mettler Toledo, USA)
7:30 pm - 8:00 pmNicola Pohl (Indiana University, USA)
"A Systems Approach to Tackling the Challenges of Carbohydrate Synthesis and Analysis"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:40 pmKlavs Jensen (Massachusetts Institute of Technology, USA)
"Automated Organic Chemistry for Screening, Optimization, and Scaling"
8:40 pm - 8:50 pmDiscussion
8:50 pm - 9:20 pmMartin Johnson (Eli Lilly and Company, USA)
"Applications of Continuous Reactors in Pharmaceutical Manufacturing"
9:20 pm - 9:30 pmDiscussion
Tuesday
7:30 am - 8:30 amBreakfast
8:30 amGroup Photo
9:00 am - 12:30 pmPrecious 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 amOlafs Daugulis (University of Houston, USA)
"New Methods for Carbon-Hydrogen Bond Functionalization"
9:30 am - 9:45 amDiscussion
9:45 am - 10:15 amDonald Watson (Univesity of Delaware, USA)
"Recent Progress in Heteroatomic Heck Reactions"
10:15 am - 10:30 amDiscussion
10:30 am - 11:00 amCoffee Break
11:00 am - 11:30 amKami Hull (University of Illinois at Urbana-Champaign, USA)
"Transition Metal-Catalyzed Amination and Amidation Reactions"
11:30 am - 11:45 amDiscussion
11:45 am - 12:15 pmVeronique Gouverneur (Oxford University, United Kingdom)
"Fluorine Chemistry: Chemical, Radiochemical and Clinical Advances"
12:15 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 pmFrom Flask to Reactor: Strategies and Tactics for Scale-Up
Discussion Leader: Sergey Pronin (University of California, Irvine, USA)
7:30 pm - 8:00 pmBrenda Burke (Gilead Sciences, Inc., USA)
"Process Chemistry Development of Ledipasvir - NS5A Inhibitor in HarvoniĀ® for Hepatitis C Treatment"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:40 pmMichael Bech Sommer (Awapatent A/S, Denmark)
"Courtroom Chemistry and Molecules with a Legal Twist"
8:40 pm - 8:50 pmDiscussion
8:50 pm - 9:20 pmRyan Shenvi (Scripps Research Institute, USA)
"Persistence"
9:20 pm - 9:30 pmDiscussion
Wednesday
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmEnlightening 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 amMelanie Sanford (University of Michigan, USA)
"Recent Developments in Catalytic C-H Functionalization"
9:30 am - 9:45 amDiscussion
9:45 am - 10:15 amTehshik Yoon (University of Wisconsin-Madison, USA)
"A General Strategy for Stereocontrol in Photochemical Reactions"
10:15 am - 10:30 amDiscussion
10:30 am - 11:00 amCoffee Break
11:00 am - 11:30 amRobert Knowles (Princeton University, USA)
"Proton Coupled Electron Transfer in Organic Synthesis"
11:30 am - 11:45 amDiscussion
11:45 am - 12:15 pmDavid MacMillan (Princeton University, USA)
"The Use of Photoredox Catalysis to Invent or Discover Unique One-Electron Mediated Reactions"
12:15 pm - 12:30 pmDiscussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session
6:00 pmDinner
7:00 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 pmApproaches for Innovative Medicines
Discussion Leader: Yi-Yin Ku (AbbVie, USA)
7:30 pm - 8:00 pmNicole Goodwin (GlaxoSmithKline, USA)
"Split Kinase Personalities: Type I and Type III Inhibitors of LIMK2"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:40 pmThomas Razler (Bristol-Myers Squibb, USA)
"Development of the Commercial Synthesis of Gamma Secretase Inhibitor BMS-708163 (Avagacestat)"
8:40 pm - 8:50 pmDiscussion
8:50 pm - 9:20 pmKris Jones (Pfizer, USA)
"Development of Ertugliflozin, a Novel SGLT2i Inhibitor: From Sugar to Co-Crystal"
9:20 pm - 9:30 pmDiscussion
Thursday
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmAdvances in Catalysis and Reaction Mechanisms
Discussion Leaders: Silas Cook (Indiana University, USA) and Matthew Beaver (Amgen, USA)
9:00 am - 9:30 amMatthew Meyer (University of California, Merced, USA)
"Exploring the Selectivity Problem in Chemistry Using Isotopes"
9:30 am - 9:40 amDiscussion
9:40 am - 10:10 amJean-Philip Lumb (McGill University, Canada)
"Driving Synthesis by Oxidation"
10:10 am - 10:20 amDiscussion
10:20 am - 10:35 amCoffee Break
10:35 am - 11:00 amJohan Wennerberg (Chemoswed AB, Sweden)
"Development of a Practical and Safe Synthesis of ABR-215062"
11:00 am - 11:10 amDiscussion
11:10 am - 11:35 amJohn Limanto (Merck Sharp & Dohme, USA)
"Development of a Long-Term Manufacturing Route to an HCV NS5b Inhibitor"
11:35 am - 11:45 amDiscussion
11:45 am - 11:55 amJill Caputo (University of Rochester, USA)
"Teaching an Old Dot New Tricks: The Use of Quantum Dots in Photoredox Catalysis"
11:55 am - 12:00 pmDiscussion
12:00 pm - 12:10 pmJustin Mohr (University of Illinois at Chicago, USA)
"Regio- and Stereocontrol with Anions and Radicals"
12:10 pm - 12:15 pmDiscussion
12:15 pm - 12:25 pmAlexandr 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 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: The Mystery of Organic Chemistry: Exploiting Surprises, Molecular Machines, and Legerdemain
Discussion Leader: Travis Remarchuk (Denali Therapeutics, Inc., USA)
7:30 pm - 8:00 pmSergey Pronin (University of California, Irvine, USA)
"New Methods and Strategies for the Synthesis of Indole Diterpenes"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:40 pmBo Qu (Boehringer Ingelheim Pharmaceuticals, USA)
"An Ideal Enantioselective Synthesis for BI 11β-HSD Inhibitor"
8:40 pm - 8:50 pmDiscussion
8:50 pm - 9:20 pmSteven Raw (AstraZeneca, United Kingdom)
"Osimertinib Mesylate: Process Development and Scale-Up of an API on the Critical Path"
9:20 pm - 9:30 pmDiscussion
Friday
7:30 am - 8:30 amBreakfast
9:00 amDeparture
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