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1,4-Oxathiins are valued for a breadth of bioactivities and are known commercial fungicides. This article explores a novel preparation of 2,3,6-trisubstituted 1,4-oxathiin-S,S-dioxides via the reaction of benzyl 1-alkynyl sulfones and aryl aldehydes under basic conditions. A total of 20 examples possessing exclusively a trans arrangement of the 2,3-diaryl substituents are exhibited; the products demonstrate a variation of functional groups on the aryl ring attached to the heterocyclic ring system.

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Cefmetazole sodium as an allosteric effector that regulates the oxygen supply efficiency of adult hemoglobin.

J Biomol Struct Dyn

September 2024

Institute of Health Service and Transfusion Medicine, Academy of Military Medical Sciences, Academy of Military Science of the Chinese People's Liberation Army, Beijing, P.R. C.

Allosteric effectors play an important role in regulating the oxygen supply efficiency of hemoglobin for blood storage and disease treatment. However, allosteric effectors that are approved by the US FDA are limited. In this study, cefmetazole sodium (CS) was found to bind adult hemoglobin (HbA) from FDA library (1338 compounds) using surface plasmon resonance imaging high-throughput screening.

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Peroxyoxalate chemiluminescence (PO-CL) is one of the most popular cold light sources, yet the drawback of aggregation-caused quenching limits their use. Here, we report a new kind of efficient bifunctional emitter derived from salicylic acid, which not only exhibits typical aggregation-induced emission (AIE) character but also has the ability to catalyze the CL process under basic conditions based on base sensitivity. By taking advantage of these unique features, we successfully confine the CL process on the surface of solid bases and provide a high-contrast visualization of CL emission.

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Aliphatic F-Radiofluorination: Recent Advances in the Labeling of Base-Sensitive Substrates*.

ChemMedChem

September 2021

Department of Drug Design and Pharmacology Faculty of Health and Medical Sciences, University of Copenhagen, Jagtvej 160, 2100, Copenhagen, Denmark.

Aliphatic fluorine-18 radiolabeling is the most commonly used method to synthesize tracers for PET-imaging. With an increasing demand for F-radiotracers for clinical applications, new labeling strategies aiming to increase radiochemical yields of established tracers or, more importantly, to enable F-labeling of new scaffolds have been developed. In recent years, increased attention has been focused on the direct aliphatic F-fluorination of base-sensitive substrates in this respect.

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Chiral Benzoins via Asymmetric Transfer Hemihydrogenation of Benzils: The Detail that Matters.

J Org Chem

May 2020

Department of Chemistry and Applied Biosciences, ETH Zurich, 8093 Zürich, Switzerland.

The synthesis of enantiomerically pure benzoins by hydrogenation of readily available benzils has been long thwarted by their base-sensitivity. We show here that an iron(II) hydride complex catalyzes the asymmetric transfer hydrogenation of benzils from 2-propanol. When strictly base-free conditions are granted, excellent enantioselectivity is achieved even with -substituted substrates, which are particularly challenging to prepare with other methods.

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