High-Speed Microwave Chemistry in Solution Phase. Applications Toward Transition Metal-Catalyzed C-P Couplings, the Kindler Reaction and Other Organic Chemistry Transformations
Poster Jul 25, 2006
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. We show applications towards a number of various synthetic protocols. As tertiary phosphines are important ligands in transition metal-catalyzed reactions a fast synthesis via direct C-P bond formation is of considerable interest.
Additional, thioamides are essential building blocks for the preperation of heterocyclic scaffolds. Here a microwave-enhanced protocol for a one-pot three-component coupling reaction is introduced.
Furthermore an application of microwave technology towards the deracemization of sulcatol is described. In particular, we show microwave-assisted high-speed Mitsunobu inversions providing rapid and racemization-free access to both (R)- and (S)-sulcatol.
Finally, we show the influence of the reaction scale to the conversion rate, depending on the formation of byproducts. All experiments have been carried out in sealed vessels using a dedicated monomode reactor (Emrys™ Synthesizer) employing microwave flash heating.
Bioluminescent Kinase Profiling Systems For Characterizing Small Molecule Kinase InhibitorsPoster
In order to profile compounds against a broad panel of kinases, in-house profiling requires rigorous kinase assay development.READ MORE
Assessment of Oral LISPRO Treatment in Ameliorating Amyloid and Tau Pathology in Transgenic Alzheimer’s Mice ModelPoster
Ionic co-crystals of lithium salicylate with organic proline (LISPRO) showed better safety and pharmacokinetic profile of lithium in plasma and brain of wild-type and transgenic Alzheimer mice model compared to lithium salts.READ MORE
CiPA Phase 2 Study: validation of an automated microelectrode array (MEA) assay of hiPSC-derived cardiomyocyte electrophysiology for cardiac safety evaluationPoster
These results support the use of hSC-CM and MEA technology for preclinical assessment of proarrhythmic risk within the proposed CiPA paradigm, and, more generally, demonstrate that automation of the CM-MEA assay can achieve high reliability and throughput for cardiac risk assessment in vitro.READ MORE