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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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Traceless Solid Phase Synthesis of Bicyclic Dihydropyrimidone Libraries Using Microwave-Assisted Cyclization Cleavage
Rolando Pérez, Doris Dallinger and C. Oliver Kappe

This poster presents a variation of the Biginelli condensation using methyl 4-chloroacetoacetate as the building block both in solution and in solid phase. This modification allows the rapid entry into a variety of bicyclic heterocyclic ring scaffolds.

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The "Victory" Reaction: A Three Component Synthesis of Pyrido[2,3-d]pyrimidines
Núria Mont, Jordi Teixidó, José I. Borrell, and C. Oliver Kappe

Here, we report our preliminary results that pyridopyrimidines 6 can be obtained in a single step as a result of a one-pot three component reaction using controlled microwave-assisted synthesis (Emrys Synthesizer).

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Microwave-Assisted Scavenging of Electrophiles Utilizing Polymer-Supported Sequestration Reagents
Doris Dallinger and C. Oliver Kappe

Recent work has reported the automated generation of a diverse library of multifunctional dihydropyrimidines (DHPMs) utilizing a microwave-mediated solution phase Biginelli three component condensation. Since most of the pharmacologically attractive DHPM derivatives are N3-acylated analogs, we became interested in developing a rapid method for accessing libraries containing this structure motif in high-throughput format.

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Tunable Carbon-Carbon and Carbon-Sulfur Cross-Coupling of Boronic Acids with 3,4-Dihydropyrimidine-2-thiones
Hana Prokopcova, Alenka Lengar and C. Oliver Kappe

Here we present a direct microwave-assisted Pd(0)-catalyzed/Cu(I)-mediated carbon-carbon cross-coupling of 3,4-dihydropyrimidine-2-thiones and 3,4-dihydropyrimidine-5-carboxylic acid thiol ester with boronic acids under Liebeskind-Srogl conditions.

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Microwave-Promoted High-Speed Negishi Cross Coupling Reaction as a Powerful Tool for Organic Synthesis
Peter Walla and C. Oliver Kappe

The aim of this research was to develop high speed microwave assisted Negishi cross coupling reaction starting from arylchlorides and to extend Fu's catalytic system (Netherton, M. R.; Fu, G. C. Org. Lett. 2001, 3, 4295) Pd2(dba)3 / tBu3P.HBF4 to microwave promoted Negishi cross couplings in solution and solid phase employing arylchlorides.

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Scientific News
2015 ACS GCI Pharmaceutical Roundtable Research Grant
Request for proposals: Greener Continuous Chemistry & Engineering Technology.
'Crumpled' Filter to Slash Energy Consumption
Scientists have developed an ultra-thin, super-strong membrane to filter liquids and gases, with the potential to cut energy consumption in industry.
Tackling Chemical Safety Rules and Regulations
Helsinki Chemicals Forum continues to lead international chemicals safety and management discussions.
Pioneering New Method to Map Enzyme Activity
Cardiff University researchers new discovery could have wide-reaching implications for the creation of manufactured goods, biofuels and therapeutic drugs.
Euro Vision turns Reality for Australia’s Iconic ‘Green Whistle’
Patients will soon benefit from a unique invention, with emergency pain killer Penthrox receiving initial regulatory approval for sale in the European and UK markets.
Gaining the Full Benefit of Microflow Electrolysis Cells
This paper sets out the factors that should be considered in seeking good performance from microflow cells for organic electrosynthesis.
Are Chemical Safety Regulations Changing Your Laboratory?
GHS changes to country chemical regulations affect everyone.
Continuous Flow of Breakthroughs for Vapourtec
Flow chemistry systems designed and manufactured by Vapourtec have recently reached the milestone of having been cited in 150 peer review publications.
A Continuous Flow System for the Measurement of Ambient Nitrogen Oxides
The proposed method can be used in industrial locations to continuously monitor ambient NOx levels and it can be automated for measuring the variation of NOx concentrations.
Accelerating Spirocyclic Polyketide Synthesis
Powerful flow chemistry techniques used for complex multi-stage synthesis of spirocyclic polyketides.
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