08:00 | Conference Registration, Materials Pick-Up, Morning Coffee |
08:45 | | Conference Chair Welcome from The Chairman of The Flow Chemistry Society Ferenc Darvas, Chairman, Flow Chemistry Society, Switzerland
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| Session Title: Conference Opening Session Chaired by Professor Aaron Beeler, Boston University |
| Session Chair: Aaron Beeler, Assistant Professor, Boston University, United States of America |
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09:00 | | Conference Chair Flow Chemistry Congress 2018 Introduction, Topics and Themes Addressed: The Field of Flow Chemistry, circa 2018 Aaron Beeler, Assistant Professor, Boston University, United States of America
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09:15 | | Keynote Presentation Making Affordable Drugs by Continuous Processes Peter Seeberger, Managing Director, Max Planck Institute of Colloids and Interfaces, Professor Freie Universität Berlin, Germany
The use of flow reactors to screen reaction conditions automatically, to discover more efficient chemical transformations and to produce affordable essential drugs. |
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09:45 | Reactions in Flow to Enable Synthesis and Medicinal Chemistry Aaron Beeler, Assistant Professor, Boston University, United States of America
In the Beeler Research Group, we are developing new technologies and approaches to enable synthesis and medicinal chemistry. The lecture will highlight developments in challenging reactions which can be used to access bioactive small molecules which are critical in our multidisciplinary and collaborative research. A common theme in our lab is the use of flow chemistry to overcome boundaries that limit reactions and to develop efficient reaction processes. Why flow chemistry? Reactions have been carried out in batch vessels for over two centuries and amazingly the tools chemists use have remained largely unchanged. As such, many of the challenges presented by batch reactions are still unsolved. Limitations such as mass transfer, heat transfer, or photon penetration can undermine the potential of a reaction when using traditional batch reactors. However, these limitations are largely mitigated in flow which enables us to reconsider the utility of many transformations for application in synthesis. Ultimately, I hope to demonstrate how flow chemistry provides us a tool for development of new and more efficient reactions that are robust, highly scalable, and provide access to complex and novel chemotypes. |
10:15 | Morning Coffee Break and Networking in the Exhibit Hall |
11:00 | “The When, Why, and How of Flow Chemistry” Timothy Jamison, Robert R. Taylor Professor and Department Head, Massachusetts Institute of Technology, United States of America
Flow chemistry has the potential to revolutionize the synthesis of organic molecules. Flow systems can reduce reaction times, increase efficiency, and obviate problems often encountered in scaling up. In addition to these important practical advantages, flow chemistry expands the “toolbox” of organic reactions available to scientists engaged in the synthesis of molecules – from small-scale experiments to large-scale production. These benefits are a direct result of several features of flow synthesis that batch synthesis typically cannot achieve, for example, the ability to control fluid flow precisely, the access to temperature and pressure regimes not usually considered to be practical, and the enhanced safety characteristics of flow chemical systems. In this lecture we will discuss some of our investigations in this area in the form of case studies, wherein a specific target or family of organic molecules has served as an inspiration for the development of new methods of organic synthesis in flow. Flow chemistry represents an important conceptual advance in the design and execution of chemical syntheses. |
11:30 | Acceleration of Drug Discovery Through the Judicious Application of Enabling Chemistry Technology Stevan Djuric, Vice President, Discovery Chemistry & Technology and Distinguished Research Fellow, AbbVie, United States of America
The talk will focus on efforts to speed up components of the Drug discovery process that can be influenced by chemistry, namely, cycle time, probability of success and cost of goods.
The following will be highlighted:
- Flow chemistry platforms for compound library production
- Fully integrated synthesis-purification- bioassay platforms
- Flow chemistry at high temperature to access key heterocyclic compounds for FBDD activities
- Reaction acceleration using microdroplet chemistry
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12:00 | Networking Lunch and Poster Viewing |
| Session Title: Emerging Technologies and Approaches in Flow Chemistry |
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13:00 | Photochemistry as an Enabling and Scalable Tool François Lévesque, Associate Principal Scientist Process Chemistry, Merck & Co., United States of America
The past ten years have seen the exponential growth of reactions promoted by visible and UV light. This has led to the discovery of very useful and highly selective transformations that were not feasible without the use of photons. Due to the unique advantages of these reactions, we foresee an increasing use of photochemistry chemistry in the synthesis and production of API. Scaling-up these reactions remains a key challenge. As most photochemical reactions require a high surface area to volume ratio for good efficiency, the utilization of these transformations on large scale is most amenable to flow. Our discussion will highlight the key parameters that need to be taken into account for an effective transition from the lab scale to preparative scale, namely geometry of the reactor, light source, photon density, path length, and residence time. Ongoing efforts by the flow chemistry team at Merck & Co., Inc. toward developing scalable photochemical reactions in flow and their application in specific case studies will be presented. |
13:30 | Tunable Chiroptical Induction Using Synchrotron-Sourced Circularly Polarized Light Amanda Evans, Scientist, Los Alamos National Laboratory, United States of America
This talk will focus on the use of circularly polarized (cp), or “chiral”, light as a supramolecular chiroptical field for the induction of asymmetry in small molecule building blocks as a continuous photochemical process. A series of batch and continuous photochemical processing experiments have been performed using synchrotron-sourced cp light as the sole source of chiroptical induction under a number of different conditions. A mechanism for asymmetry generation in these small molecule building blocks in solvent and methods for enhancing the initial selectivities observed will be discussed. Predictive approaches for describing the behavior of similar small molecules will also be presented. |
14:00 | The Intersection Between Technology and Need D. Tyler McQuade, Professor, Virginia Commonwealth University, United States of America
I will present current efforts and success stories related to the Medicines for All Institute (M4All). M4All’s objective is to use advanced chemistry and technology (flow chemistry) to realize low cost manufacturing process for critical medicines. |
14:30 | Afternoon Coffee Break and Networking |
15:15 | Fully Continuous Mulit-Step GMP Synthesis of Drug Substance in a Fume Hood Facility Joel Calvin, Research Scientist, Eli Lilly and Company, United States of America
Development and implementation of flow process to make drug substance that include a Buchi operation for solvent exchange, Grignard formation using magnesium in a CSTR, a Negishi reaction in a solids handling PFR and a continuous anti-solvent/cooling crystallization of API. The process was run at our manufacturing small volume continuous facility. |
15:45 | New Continuous Flow Synthetic Methods with Highly Reactive Intermediates Hélène Lebel, Professor, Department of Chemistry, University of Montreal, Canada
Continuous flow technology offers many advantages, including the safe manipulation of highly reactive intermediates. As such, a number of methods for the preparation and the use of diazo reagents in continuous flow have been described in the literature. Another class of highly reaction intermediates that benefit from continuous flow technology are aliphatic diazonium intermediates. The Lebel group has shown that aliphatic diazoniums can be in-situ generated from an amine and a nitrite reagent in the presence of an acid. The reaction conditions are compatible with a large variety of functional groups. The trapping of aliphatic diazoniums with carboxylates, electron rich aromatics and other nucleophiles afforded various synthetic compounds in high yields. The optimization details and the scope of this methods will be described in this presentation. |
16:15 | Chemistry in Low Earth Orbit Kenneth Savin, Sr. Associate Program Scientist, CASIS (Center for the Advancement of Science In Space), United States of America
The opportunity to do chemical research on the International Space Station-National Lab will be presented by CASIS (the Center for the Advancement of Science In Space). The International Space Station provides a unique environment to perform research that can benefit your own efforts and we shall describe the lab and some of the types of research that has been done on station. In addition to chemical studies performed on station, we will briefly focus on key chemistries that are incorporated into the Space Station Systems. The hope is that individuals will come away with a new appreciation for the on-station environment and consider developing their own research to be performed on the International Space Station. |
16:45 | Flow Chemistry Approaches to Nano- and Micro- Particle Synthesis Andrew Mansfield, Flow Chemistry Leader, Syrris
The widespread adoption of flow chemistry for organic synthesis is well known. In more recent years, there has been a huge growth in research into materials applications in flow. This talk will explore different reactions in nano- and microparticle synthesis with a look into the different approaches that can be used depending on what type of particle is being produced. It is also important to explore the relevant application areas for the materials research from metal nanoparticles, quantum dots through to drug delivery systems using API encapsulates polymer micro particles. |
17:15 | Research Towards Automated Continuous Flow Peptide Synthesis Duncan Guthrie, Director & Owner, Vapourtec, Ltd.
Today, the focus of therapeutic pharmaceuticals is beginning to shift away from small molecular medicines and towards larger, peptide based treatments. Peptides have enormous potential as medicinal compounds. They are highly specific and often potent. Solid phase approaches to peptide synthesis are attractive, however challenges remain. This presentation describes the key achievements in Vapourtec’s work towards gaining benefit from continuous flow approaches to solid phase peptide synthesis. |
17:45 | | Keynote Presentation C-H Functionalization Chemistry in Flow Huw M. L. Davies, Asa Griggs Candler Professor of Chemistry, Emory University, United States of America
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18:30 | Close of Day 1 of the Conference. |