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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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Scalability of Heterocyclic Microwave-Assisted Transformations From Batch to Continuous Flow - A Case Study
Jennifer M. Kremsner, Bimbisar Desai, Alexander Stadler and C. Oliver Kappe

Herein we present a case study on the small to large scale microwave-assisted synthesis of the DHPM 4 under batch and continuous flow conditions in monomode and multimode cavities.

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High-Speed Transition Metal-Catalyzed Chemistry Promoted by Microwave Irradiation
Toma Glasnov, Peter Walla, Alexandler Stadler, Alenka Lengar,Bimbisar Desai, Bogdan Khanetskyy, Doris Dallinger and C. Oliver Kappe

When using traditional heating under reflux conditions many transition metal-catalyzed C-C and C-X bond forming reactions typically need hours or days to reach completion. Fast and reliable microwave protocols are therefore very much needed for speeding up transformations in the field of homogeneous catalysis, taking into account the advantages of microwave heating – rapid transfer of energy and inverted temperature gradients, by increasing the lifetime of the catalyst, i.e. eliminating the wal

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Rapid Generation of Polymer-Bound Enones by Microwave-Assisted Solid-Phase-Synthesis
Gernot A. Strohmeier and C. Oliver Kappe

We have shown that two important reactions in solid-phase synthesis can be easily accelerated by the assistance of microwave irradiation. Acetoacetylations were performed in 1-5 minutes instead of 18 hours. Knoevenagel condensations were acceptably reduced from 1-3 days to one hour. The increased temperatures didn’t reduce the purity of the final products.

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Showing Results 41 - 50 of 61
Scientific News
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.
Syrris Atlas has the Midas Touch with Nanoparticles
Spanish biotechnology company Midatech Biogune is taking advantage of our Atlas Potassium reactor systems to produce custom-made functionalized gold nanoparticles for medicinal use.
Simple, Rapid and Effective Method for Ammonia Determination
Researchers have a developed a modern, miniaturized and economic flow system to overcome problems of using Nessler's reagent for ammonia determination.
Preparation of Phosphines Through C–P Bond Formation
This article reviews some of the most important C–P bond formation strategies, organizing them according to the hybridization of carbon in the newly formed C–P bond.
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.
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