Publications by authors named "E Van der Eycken"
Schizophrenia (SCZ), bipolar (BD) and major depression disorder (MDD) are severe psychiatric disorders that are challenging to treat, often leading to treatment resistance (TR). It is crucial to develop effective methods to identify and treat patients at risk of TR at an early stage in a personalized manner, considering their biological basis, their clinical and psychosocial characteristics. Effective translation of theoretical knowledge into clinical practice is essential for achieving this goal.
View Article and Find Full Text PDFWe herein report the efficient synthesis of peptide-benzazepine conjugates from Lys-based peptides and acroleins via Rh(III)-catalyzed double C-H activation. This reaction features mild reaction conditions, broad scope, high atom and step economies, and excellent chemo- and site selectivity. The synthetic utility of this strategy is further demonstrated by scale-up experiments and product derivatizations, including diverse late-stage ligations based on the aldehyde moiety.
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- The Minisci reaction is an effective method for directly modifying heterocyclic molecules through C-H functionalization, relying on radical chemistry.
- It has gained popularity because its results are predictable based on the types of radicals and heterocycles used.
- The review discusses recent strategies, particularly the use of continuous flow techniques, to scale up this reaction for drug development purposes.
Article Synopsis
- - The study demonstrates the use of inactivated alkyl boronic acids (BAs) as effective partners in a photocatalyzed Suzuki-Miyaura reaction without needing external activators or strong oxidants.
- - It proposes a unique activation pathway for BAs involving a radical transfer between a bromine radical and the boron atom's empty p-orbital, which differs from traditional methods that rely on tuning oxidation potential.
- - The findings are backed by control experiments and density functional theory (DFT) calculations, introducing a new halogen radical transfer (XRT) mechanism for the reaction.
In this study, we present an inexpensive, stable, and easily available boryl radical source (BPhNa) employed in a Halogen Atom Transfer (XAT) methodology. This mild and convenient strategy unlocks the use of not only alkyl iodides as radical precursors but also of the more challenging alkyl and aryl bromides to generate C-centered radicals. The generated radicals were further engaged in the -Markovnikov hydroalkylation of electronically diverse styrenes, therefore achieving the formation of C(sp)-C(sp) and C(sp)-C(sp) bonds.
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