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Agenda

Day One – 8th April

08:00

Registration

09:00

Microwave Synthesis
Session Chair: Oliver Kappe, Associate Professor of Chemistry, University of Graz

09:05

Towards New Methodologies for the Synthesis of Biologically Interesting Pyrimidine Derivatives
Maurizio Botta, Professor, University of Siena
An overview on the application of modern techniques (e.g. solid- and solution-phase synthesis, parallel synthesis, microwave assisted techniques) to the synthesis of highly substituted pyrimidine derivatives will be given.

09:35



Microwaves as Tools for Expedient Chemical Synthesis
Catherine Smith, PhD Student, University of Cambridge
Microwaves have proven tremendously valuable in the synthesis of small molecule targets. The incorporation of other enabling technologies such as immobilized reagents and catalysts further enhances the efficiency of many microwave-promoted reactions. This talk will present a synopsis of our group's experiences using these approaches in both batch and flow mode microwave syntheses of novel heterocyclic compounds.

10:05

Coffee & Networking in Exhibition Hall

10:50

Microwave Technology for High-Throughput Synthesis Applications
Marcus Koppitz, Scientist, Bayer Schering Pharma
Multimode microwave systems in combination with suitable pressure blocks allow for true parallel synthesis of compound arrays, thereby significantly speeding up the production process. The presentation describes synthesis setup as well as its integration into the overall process of compound production to support drug discovery projects.

11:20

Microwave Combinatorial Parallel and Non Parallel Synthesis of Novel Arylpiperazine Derivatives as 5-HT1A Serotoninergic Agents
Vincenzo Santagada, Professor, University of Naples 
An easy and convenient microwave-assisted synthesis of indolic arylpiperazine derivatives was developed with parallel and non-parallel combinatorial methods. This allows the obtaining of a small library of compounds with just one reaction and purification step.

11:50

Design and Synthesis of Ring-Fused 2-Pyridones
Fredrik Almqvist, Professor, Umeå University
Highly substituted ring-fused 2-pyridones are excellent scaffolds for the development of novel antibacterial agents, pilicides, that target bacterial virulence. The design synthesis and further functionalisation of these heterocycles and their antivirulence properties will be presented.

12:20

Lunch & Poster Viewing

14:00

Organic Chemistry
Session Chair: Fredrik Almqvist, Professor, Umeå University

14:00

Improving Organic Synthesis by Microwave Irradiation - New Trends
Oliver Kappe, Associate Professor, University of Graz
This presentation will focus on the integration of microwave synthesis with other enabling technologies such as parallel processing, reaction optimization by Design of Experiment and continuous flow chemistry. Several chemistry examples derived from a drug discovery context will be presented.

14:30

Microwave Assisted Multi-Component and Domino Syntheses of Carbo- and Heterocycles
Thomas Müller, Professor, University of Duesseldorf
Microwave assisted ransition metal catalyzed reactions, in combination with condensation chemistry, are new, straightforward entries to diversity-oriented multi-component and domino syntheses of heterocycles and complex structural scaffolds in a one-pot fashion.

15:00

Coffee & Networking in Exhibition Hall

15:45

Microwaves in Metal-Free and Metal-Catalyzed Organic Reactions
Carsten Bolm, Professor, RWTH Aachen
The lecture will focus on the application of microwave irradiation in three organic reactions: 1. The synthesis of quinolones, 2. organocatalytic asymmetric Mannich reactions, and 3. ruthenium-catalyzed alkyne hydrations.

16:15

Carbon Nanostructures Towards Materials for Molecular Electronics
Fernando Langa, Professor, University Castilla-La Mancha
Carbon nanostructures (fullerenes, carbon nanotubes) can be considered among the most promising materials in molecular electronics. Solubility and modulation of their electronic properties can be achieved by functionalization. Recent examples of functionalized carbon nanostructures for molecular electronics will be presented.

16:45

Towards Unsolved Problems at Applications with Microwaves
Bernd Ondruschka, Director, University of Jena
The present time is determined by broad acceptance of microwaves as thermal heating source for syntheses and material separations. Important input for understanding of the phenomenon microwaves within the chemistry and/or chemical engineering is the comprehensive knowledge of the fundamental regularities and laws of natural sciences, material sciences, physics, chemistry and engineering.

17:15

The Benefits of Automation in Microwave Assisted Workflows
Michael Schneider, Vice President, Chemspeed Technologies

17:45

SOPHAS New Generation Automated Solid Phase Synthesis
Werner Zinsser, CEO, Zinsser Analytic

18:15

Drinks Reception and Networking in Exhibition Hall

 

Day Two – 9th April

09:00

Flow Chemistry
Session Chair: Ferenc Darvas, President, Thales Nanotechnology, Hungary

09:05

Chemistry in a Tube: Flow Synthesis
Ian Baxendale, Professor, University of Cambridge
Flow synthesis has become a very popular concept that is destined to revolutionise the future of synthetic chemistry. However, in order to achieve the full potential offered by these flow-based techniques, it is necessary both to develop versatile reactors and to couple this technology with a fundamental understanding of the chemistry. In this talk we describe the evolution of flow chemistry within our group. 

09:35

Microwaves, Heterocycles and Flow Reactors
Mark Bagley, Senior Lecturer, University of Cardiff
Microwave irradiation accelerates many processes for the synthesis and functionalization of heterocycles. The performance of a novel continuous flow microwave reactor and its comparison with traditional batch technology and other proprietary flow apparatus has been established for a range of transformations.

10:05

Coffee & Networking in Exhibition Hall

10:50

Microreactors as Tools for Synthetic Chemists
Peter H. Seeberger, Professor, Swiss Federal Institute of Technology (ETH)
Flow through systems have become increasingly interesting to practitioners of organic synthesis. Described is the use of different microreactor systems to optimize reactions conditions, to carry out reactions otherwise too dangerous and to create pharmaceutically active compounds.

11:20

Microfluidic Closed Loops - A New Paradigm in Drug Discovery
Brian Warrington, Director, BB Consultants
An efficient, microfluidic strategy for lead identification and optimisation is described. Bench top integration of the chemistry, biology and informatics modules that may overcome at low cost the inefficient logistics and restricted diversity shortcomings of the current paradigms are illustrated.

11:50

Applications of Flow Chemistry in Drug Discovery
Christopher Selway, Lead Scientist, Pfizer
Over the last year, an expanding selection of instrumentation for flow synthesis aimed at the medicinal chemist has allowed pharma to investigate the applications of this methodology.

12:20

Lunch & poster viewing

14:00

Closed-Loop Dynamic Combinatorial Flow Chemistry
Sven Schroeder, Professor, University of Manchester
This presentation will discuss how, with the use of spatially resolving in situ probes, the patterns of product formation in flow reactors can be visualised and optimised towards the desired product.

14:30

Investigating Flow Chemistry as a Tool for Iterative Parallel Synthesis
Paul Tempest, Group Leader, Merck
We have installed an AFRICA (Automated Flow Reaction and Incubation Control Apparatus) system in our labs and have run a series of increasingly complex synthetic tasks to both validate the hardware and assess whether flow chemistry is a viable tool for our purposes.  These experiments, beginning with simple recovery tests and ending with multiple component condensation reactions will be presented.

15:00

Coffee & Networking in Exhibition Hall

15:45

Application of Flow Chemistry Under Supercritical Conditions
Ferenc Darvas, President, Thales Nanotechnology 
Flow reactors operating on high pressure, high temperature, optionally pre-packed with catalysts, reagents, or scavengers are presented to perform hydrogenation, coupling reactions, and catalytic isomerization under supercritical conditions. Optimizing selectivity by residence time control or using scCO2 for dilution are discussed.

16:15

Meso Scale Chemistry Using an Integrated Benchtop Flow Reactor
Mark Ladlow, Chief Scientific Officer, Uniqsis

16:45    

Close of Conference