The synthesis of small rings by functionalization of C(sp(3) )-H bonds remains a great challenge. We report for the first time a copper-catalyzed [1+1+1] cyclotrimerization of acetophenone derivatives under mild reaction conditions. The reaction has a broad scope for the stereoselective synthesis of cyclopropanes by trimerization of acetophenone. The developed transformation is based on an extraordinary copper-catalyzed cascade process that allows saturated carbocycles to be obtained for the first time by cyclotrimerization through functionalization of C(sp(3) )-H bonds. The cascade of sixfold C(sp(3) )-H bond functionalization allows the synthesis of cyclopropanes in a highly stereoselective approach.
We have developed a glycosyl radical-based synthesis of -alkyl glycosides through a deoxygenative Giese addition-reduction-cyclization cascade, in which readily available 1-hydroxy carbohydrates serve as precursors for glycosyl radicals and aryl alkenes function as radical acceptors. This reaction not only provides an effective method for accessing a previously underexplored class of functionalized cyclopropanes but also enhances the application of Giese addition in the synthesis of -alkyl glycosides by derivatizing the radical intermediate generated through polar cyclization to yield a cyclopropane.
Purpose: Ciprofol is a novel intravenous anesthetic that has been increasingly used in clinical anesthesia and sedation. Studies suggested that ciprofol reduced oxidative stress and inflammatory responses to alleviate cerebral ischemia/reperfusion (I/R) injury, but whether ciprofol protects the heart against I/R injury and the mechanisms are unknown. Herein, we assessed the effects of ciprofol on ferroptosis during myocardial I/R injury.
Dipartimento di Scienze Chimiche e Geologiche, Università degli Studi di Cagliari, Complesso Universitario di Monserrato, 09042, Monserrato (Cagliari), Italy.
The continuous flow telescoped synthesis of 1,1-cyclopropane aminoketones was achieved by optimizing the photocyclization of 1,2-diketones to 2-hydroxycylobutanones (HCBs) and their reaction with aryl- and alkylamines, tandem condensation C4-C3-ring contraction reaction. With the achieved operational conditions, we were able to obtain a library of cyclopropylamines with good chemical yields, high productivity, and short residence times.
Novel Co/NC heterogeneous catalysts were prepared by simply employing self-made Co/Zn-ZIF (zeolitic imidazolate framework) through pyrolysis. The samples were characterized by XRD, XPS, Raman, TEM and BET, and were successfully applied in a cyclopropanation reaction with a yield of 85%. Furthermore, this one-pot synthesized catalyst could be recycled several times without apparent deactivation.
Laboratory of Chemical, Galenic and Pharmacological Development of Medicines (LR12ES09), Faculty of Pharmacy of Monastir, University of Monastir, Monastir, Tunisia.
Background: Phosphodiesterase-4 is an enzyme that regulates immune responses and contributes to the development of psoriasis. Dipyridamole and roflumilast function as phosphodiesterase-4 inhibitors, reducing pro-inflammatory cytokine expression. The aim was to evaluate the anti-psoriatic effect of the topical administration of dipyridamole and roflumilast nanoemulgel combination on imiquimod-induced psoriasiform skin inflammation in rats.
