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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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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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Microwave-Assisted Three-Component One-Pot Synthesis of Highly Substituted 2-Pyridinones
Behrooz H. Yousefi, Nikolay Yu. Gorobets and C. Oliver Kappe

Pyridone and quinolone analogous are known to possess valuable biological activities. The aims of this research were the development of a one-pot multi-component synthesis of 2-pyridinone libraries and the application of controlled microwave heating to gain rapid access to diverse 2-pyridinones utilizing CH-acidic carbonyl compounds 4, DMFDMA 5 and methylene active nitriles.

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Scaffold Decoration at the N3-Position of Dihydropyrimidine Derivatives by Microwave-Assisted Solution Phase Synthesis
Doris Dallinger and C. Oliver Kappe

In the library synthesis of N3-acylated DHPMs, different scavenging techniques using polymer-supported sequestration agents are described for the purification steps. In both synthesis and purification microwave flash heating was utilized, reducing reaction times from hours to minutes. In order to introduce novel diversity in the N3-position of the DHPM-scaffold, N3-arylations were performed by applying classical Cu (I)-catalyzed Goldberg reaction conditions under microwave heating.

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Showing Results 31 - 40 of 54
Scientific News
Catalysts That Mimic Enzymes Could Revolutionize Pharmaceutical Manufacturing
Structures made of polymer chains allow the catalysts to work in water.
High Temperature Synthesis Using Heating Blocks
Asynt DrySyn MULTI heating block systems are being utilised to support ground breaking synthetic research in photovoltaics, water splitting and nanoimaging.
Lonely Bacteria are More Likely to Become Antibiotic-resistant
Scientists from the University of Manchester have discovered that microbes in smaller groups are more likely to mutate, resulting in higher rates of antibiotic resistance.
Lab Scale Manufacturing Using Continuous Crystallization
A new METTLER TOLEDO On-demand webinar explores recent research that could revolutionize pharmaceutical production.
MIT Chemists Devise Novel Way to Manufacture Peptide Drugs
New, fast synthetic method enables manufacture of peptides in hours, which could boost drug development.
The Future Of Photochemistry
The Vapourtec UV-150 offers potential routes for novel compounds and building blocks together with possible new manufacturing processes.
Continuous-Flow Heck Synthesis of 4-Methoxybiphenyl and Methyl 4-Methoxycinnamate in scCO2 Expanded Solvent Solutions
This paper reports the Heck reaction between 4-iodoanisole and either styrene or methyl acrylate in a continuous flow reactor.
Silica: An Efficient Catalyst for One-Pot Regioselective Synthesis of Dithioethers
Researchers demonstrate that the choice of silica gel, either dry or moistened, could lead to highly selective pathways for the preparation of different dithioethers.
Flow Synthesis of Phenylserine using Threonine Aldolase Immobilized on Eupergit Support
Researchers from Eindhoven University of Technology have made the first step towards a critical view on the commercial potential for high-priced pharmaceutical products using enzymatic microreactor technology.
One-Step Synthesis of Pyridines and Dihydropyridines in a Continuous Flow Microwave Reactor
Microwave-assisted synthesis has revolutionized many processes in recent years as a valuable alternative to the use of conductive heating.
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