Literature Survey Part A: Transition Metal‐Catalyzed Reactions

Kappe, C. Oliver; Stadler, Alexander; Dallinger, Doris

doi:10.1002/9783527647828.ch5

Microwaves in Organic and Medicinal Chemistry

2012

DOI: 10.1002/9783527647828.ch5

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Literature Survey Part A: Transition Metal‐Catalyzed Reactions

C. Oliver Kappe

Alexander Stadler

Doris Dallinger

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Cited by 2 publications

References 610 publications

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Advances in microwave-assisted synthesis and the impact of novel drug discovery

Berrino

2018

Expert Opinion on Drug Discovery

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Microwave (MW)-assisted synthesis of biologically active compounds has received a lot of attention in the last decades due to the advantages that such a technique offers compared to traditional heating procedures. Areas covered: The authors provide a focused review on the recent applications of this technique for drug design purposes. MW syntheses have been used for designing libraries of compounds, in combinatorial and multicomponent approaches, for lead optimization, as well as for forcing reactions which do not occur or occur in low yields using traditional methods. Expert opinion: This technique offers significant advantages over the traditional heating due to the fact that the reaction time is shortened, the possibility to have concurrent side reactions is decreased and the use of smaller amounts of polluting solvents is also reduced. However, no significant technical advances have been reported for MW-assisted devices in the last years, with the important novelty being only in the type of reactions/compounds that have been investigated and synthesized using the MW heating approach.

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Advances in microwave-assisted synthesis and the impact of novel drug discovery

Berrino

2018

Expert Opinion on Drug Discovery

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An Automated Microwave-Assisted Synthesis Purification System for Rapid Generation of Compound Libraries

Searle

Sarris

2016

SLAS Technology

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A novel methodology for the synthesis and purification of drug-like compound libraries has been developed through the use of a microwave reactor with an integrated high-performance liquid chromatography-mass spectrometry (HPLC-MS) system. The strategy uses a fully automated synthesizer with a microwave as energy source and robotic components for weighing and dispensing of solid reagents, handling liquid reagents, capper/crimper of microwave reaction tube assemblies, and transportation. Crude reaction products were filtered through solid-phase extraction cartridges and injected directly onto a reverse-phase chromatography column via an injection valve. For multistep synthesis, crude products were passed through scavenger resins and reintroduced for subsequent reactions. All synthetic and purification steps were conducted under full automation with no handling or isolation of intermediates, to afford the desired purified products. This approach opens the way to highly efficient generation of drug-like compounds as part of a lead discovery strategy or within a lead optimization program.

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Literature Survey Part A: Transition Metal‐Catalyzed Reactions

Cited by 2 publications

References 610 publications

Advances in microwave-assisted synthesis and the impact of novel drug discovery

Advances in microwave-assisted synthesis and the impact of novel drug discovery

An Automated Microwave-Assisted Synthesis Purification System for Rapid Generation of Compound Libraries

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