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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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Polymer-Bound Fused N -(1-Chloroalkyl)Azinium Chlorides As Synthetic Equivalents Of Aldehydes.
Jean Jacques Vanden Eynde, Annie Mayence and Ernst Anders.

A few years ago the first multi-component synthesis of N-(1 -haloalkyl) pyridinium halides from a thionyl halide, pyridine, and an aldehyde was described. Since that time, we have widely demonstrated that such salts can be considered as valuable synthetic equivalents of the starting aldehydes for the preparation of various classes of nitrogen heterocycles.

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Application of Microarrays in Process Analytical Technologies A First Step Towards Real Time Product Release
Streefland M, van de Waterbeemd B, vander Pol LA, Beuvery EC, Martens DE,Tramper J

Application of microarrays during process development helps to gain insight in biological processes involved in product formation, increasing process understanding.

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From Medicinal Plants to Bioactive Drugs
Ilaria Lampronti, Mahmud T.H. Khan, Antoine M. Saab, Elisabetta Lambert, Letizia Penolazzi, Roberta Piva and Roberto Gambari

The aim of our study was to analyze the antiproliferative activity effects on human tumor cell lines and the differentiating activity on human erythroleukemic K562 cells of different extracts derived from medicinal plants of Bangladesh and Lebanon.

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Showing Results 41 - 50 of 55
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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