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New Accessories for High Throughput and Combinatorial Approach in a Microwave Batch Reactor
Alexander Stadler, Thomas Karner, Matthias Treu

A unique sealable well-plate system is introduced allowing screening reactions in a 8x6 well format with operation limits of 200°C and 20 bar and a reaction volume of 0.3 mL per well. An appropriate turntable enables to proceed up to 4 of these SiC well plates in one run resulting in 192 parallel reactions at a time. Reaction control is achieved by sensing the IR temperature of the plate surface.

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Microwave Accelerated Heterogeneous Catalysis – Flow-Through Reactor Concept and Application
T. Glasnov, K. Mennecke, R. Cecillia, U. Kunz, A. Kirschning and C.O. Kappe,

Flow-through processes in organic synthesis become more important as an enabling technology for a cost effective and convenient method. This requires appropriate reactors with functionalities for organic reactions. In this project noble metal-loaded polymer/carrier reactors able to be operated in a microwave field were investigated. By application of a microwave field metal sites are heated whereas the polymer/carrier material remains transparent to irradiation.

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Phase Tranformation of Sodium Carbonate to Monohydrate
A. Shaikh, A.D. Salman, S. Mcnamara, G, Littlewood and M.J. Hounslow

Sodium carbonate is the most widely used chemical compound in the world. The 50% of this used in glass industry is in the form of dense sodium carbonate. The process of transformation of sodium carbonate to sodium carbonate monohydrate is the key step in the production of dense sodium carbonate. In this present work systematic experiments were conducted by using online in-situ measurement techniques. It is shown that the kinetics of phase transformation process is highly temperature dependant.

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Synthesis of 4,5-dihydroisoxazoles from N-nitroso-4,5 dihydropyrazoles under Microwave Irradiation
Kostikov R.R., Stepakov A.V., Galkin I.A and Molchanov A.P.

4,5-Dihydroisoxazoles have been used as key intermediates in the synthesis of a bioactive molecules and are found in pharmaceutical agents such as glycoprotein IIb/IIIa (GPIIb/IIIa) inhibitors and human leukocyte elastase inhibitors. In the present work 4,5-dihydroisoxazoles have been prepared by thermal removal of nitrogen from N-nitroso-4,5-dihydropyrazoles under microwave irradiation.

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The Effect of Microwave Irradiation Towards Carbodiimide-Mediated Esterifications on Solid Phase
Alexander Stadler and Oliver Kappe

A number of publications have reported the coupling of carboxylic acids to Merrifield resin via the cesium salt method and the esterification of Wang resin using carbodiimide either via the isourea method or the symmetrical anhydride method. Reaction times using conventional conditions have been reported to be rather long so we have investigated the effects of microwave irradiation towards both of these reactions using benzoic acid derivatives.

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Rapid Scaffold Decoration of Dihydropyrimidine Derivatives by Microwave-Assisted Solution Phase Synthesis
Doris Dallinger, Alenka Lengar, Bogdan Khanetskyy, Bimbisar Desai and C. Oliver Kappe

In recent work we have reported the generation of a diverse library of DHPMs, employing an automated, sequential microwave-assisted solution phase strategy. We now present the high-speed microwave scaffold decoration around the DHPM heterocyclic core exploiting the diversity on at least six positions.

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Microwave-Assisted Organic Synthesis in Near-Critical Water at 300°C. A Proof-of-Concept Study
Jennifer M. Kremsner and C. Oliver Kappe

Microwave-assisted organic synthesis in near-critical water (NCW) in the 270-300 °C temperature range has been investigated in a dedicated multimode microwave reactor utilizing heavy-walled quartz reaction vessels. Several different known transformations such as the hydrolysis of esters or amides, the hydration of alkynes, Diels-Alder cycloadditions, pinacol rearrangements, and the Fischer indole synthesis were successfully performed in microwave-generated NCW without the addition of an acid

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Microwave-Promoted Hetero-Diels-Alder Reactions of 2(1H)-Pyrazinones in Ionic Liquid Doped Solvents and on Solid Support
Nadya Kaval, Erik Van der Eycken and C. Oliver Kappe

The readily available and broadly functionalized 2-azadiene system of the 2(1H)-pyrazinones easily undergo inter- and intramolecular Diels-Alder reactions with a wide range of dienophiles providing convenient routes to specifically substituted heterocycles. The reactions in this series are known to be rather sluggish, requiring long reaction times, high temperatures and even sometimes high pressures. Since speed is generally recognized as an important factor in high-throughput synthesis, we have

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High-Speed Microwave Chemistry in Solution Phase. Applications Toward Transition Metal-Catalyzed C-P Couplings, the Kindler Reaction and Other Organic Chemistry Transformations
Alexander Stadler, Oleksandr I. Zbruyev and C. Oliver Kappe

Speeding-up of organic reactions using microwave dielectric heating has attracted increasing importance in recent years. This poster presents applications towards a number of various synthetic protocols including a microwave-enhanced protocol for a one-pot three-component coupling reaction.

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Scientific News
Solvent-free, Catalyst-free Peracetylation of Natural Products
In this study, a tunable microwave-assisted method for the solvent-free and catalyst-free peracetylation of natural products was developed.
Sonochemical Reactors
A critical analysis of the underlying mechanisms for intensification, available reactor configurations and overview of the different applications exploited successfully are presented.
Economical and Scalable Synthesis of 6-amino-2-cyanobenzothiazole
An economical and scalable synthesis of ACBT is presented, along with advantages for scale-up over previously reported routes.
Peer Review is in Crisis, But Should be Fixed, Not Abolished
After the time to get the science done, peer review has become the slowest step in the process of sharing studies, and some scientists have had enough.
3D-Printing in Science: Conference Co-Staged with LABVOLUTION
LABVOLUTION 2017 will have an added highlight of a simultaneous conference, "3D-Printing in Science".
Cutting the Cost of Drug-Building Chemicals
EPFL scientists have developed a method to produce aryl-containing amines in a cheap and easily scalable way.
How Cloud Connectivity Can Combat the Reproducibility Crisis
This infographic explains the reproducibility crisis, and how cloud connectivity can help overcome this problem.
Porphyrins as Catalysts in Scalable Organic Reactions
This review covers the most relevant scalable porphyrin-catalysed procedures, showing how these compounds represent broad applications in chemistry.
What Makes a Good Scientist?
It’s the journey, not just the destination that counts as a scientist when conducting research.
Injecting New Life into Old Antibiotics
A new fully synthetic way to make a class of antibiotics called macrolides from simple building blocks is set to open up a new front in the fight against antimicrobial drug resistance.
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