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The Effect of Microwave Irradiation Towards Carbodiimide-Mediated Esterifications on Solid Phase
Alexander Stadler and Oliver Kappe

A number of publications have reported the coupling of carboxylic acids to Merrifield resin via the cesium salt method and the esterification of Wang resin using carbodiimide either via the isourea method or the symmetrical anhydride method. Reaction times using conventional conditions have been reported to be rather long so we have investigated the effects of microwave irradiation towards both of these reactions using benzoic acid derivatives.

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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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Showing Results 31 - 40 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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