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Wednesday, September 17, 2014
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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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Microwave Assisted Synthesis of Substituted 2(1H)-Quinolones as Maxi-K+ Channel Openers
Toma Glasnov, Wolfgang Stadlbauer and C. Oliver Kappe

Here we present a novel synthetic strategy for synthesis of 4-aryl-2(1H)-quinolone lead compounds for the treatment of male ED. The MW-reaction protocols are high-diversity generating, flexible, amenable to high-speed MAOS, scalable and involve commercially available building blocks. Our approach for making the 4-arylquinolones includes a cyclization step, chlorination/hydrolysis, Suzuki C-C coupling,[8] bromination, and finally a Heck reaction, all under microwave conditions.

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Automated Generation of a Dihydropyrimidine Library Using Sequential Microwave-Assisted Synthesis
Alexander Stadler and C. Oliver Kappe

The aim of this study was to generate a library of dihydropyrimidines utilizing rapid automated sequential microwave-assisted chemistry.

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Interfacing Microwave Synthesis with Enabling Technologies in Drug Discovery
Doris Dallinger and C. Oliver Kappe

Here we report on the rapid synthesis/decoration of privileged heterocyclic scaffolds, namely the dihydropyrimidine (DHPM) scaffold, by applying microwave heating in conjunction with PASP approaches.

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Showing Results 41 - 50 of 58
Scientific News
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.
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.
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