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We have successfully developed P(NMe)-mediated reductive cyclopropanation, which provides a new, facile, and efficient protocol for the synthesis of cyclopropyl carbocyclic nucleosides, wherein the cyclopropyl group is linked to the nucleobase via a methylene group. This method utilizes safe, commercially available α-keto esters for metal-free cyclopropanation under mild conditions with high yield and diastereoselectivity, demonstrating broad applicability and practical utility in carbocyclic nucleoside synthesis.
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http://dx.doi.org/10.1021/acs.joc.5c01138 | DOI Listing |
J Integr Neurosci
August 2025
Department of Anesthesiology, The Fourth Affiliated Hospital of Harbin Medical University, 150001 Harbin, Heilongjiang, China.
Background And Purpose: Ciprofol, a novel intravenous anesthetic, has been shown to exert protective effects against ischemic stroke, a leading cause of death and disability; however, its molecular mechanisms remain unclear. This study aimed to explore the molecular mechanisms underlying the neuroprotective effects of ciprofol using metabolomics.
Methods: This study used a middle cerebral artery occlusion (MCAO) rat model to simulate cerebral ischemia-reperfusion injury (CIRI).
Org Lett
September 2025
Henan Provincial Engineering and Technology Research Center for Precise Synthesis of Fluorine-Containing Drugs. College of Chemistry and Chemical Engineering, Anyang Normal University, Anyang, 455000, P. R. China.
In this work, we report a novel I-mediated ring-opening -difunctionalization of cyclopropyl alcohols with enaminones for the first time. The selective [3 + 2] annulation instead of [3 + 3] annulation under metal-free conditions enables a straightforward and efficient synthesis of structurally important 2,4-diacylpyrroles. Notably, this methodology dispenses with metal catalysts, proceeds under mild reaction conditions, and features not only simple operation but also suitability for gram-scale preparation and late-stage functionalization of complex bioactive molecules.
View Article and Find Full Text PDFDrug Des Devel Ther
September 2025
Zhejiang University School of Medicine, Hangzhou, People's Republic of China.
Background: Depression is a complex neuropsychiatric disorder involving neuroinflammation, synaptic dysfunction, and neurotransmitter dysregulation. Recent studies have highlighted the therapeutic potential of short-acting anesthetics in the treatment of depression. Ciprofol, a novel intravenous anesthetic with rapid onset and recovery, shows promise, although its antidepressant mechanisms remain underexplored.
View Article and Find Full Text PDFChemistry
August 2025
INSA Rouen Normandie, Univ. Rouen Normandie, Univ. Caen Normandie, ENSICAEN, CNRS, Normandie Univ., Institut CARMeN, Rouen, F-76000, France.
The ring expansion of α-cyclopropyl diazoacetates into cyclobutenoates upon irradiation at 425 nm was reported. This method allowed an access to a large array of cyclobutenoates as a mixture of regioisomers. The products were isolated in moderate to excellent yields (17% to 75%) and moderate to good regioisomeric ratio (55:45 to 82:18).
View Article and Find Full Text PDFJ Org Chem
August 2025
College of Chemistry and Chemical Engineering, Xinyang Normal University, Xinyang, Henan 464000, China.
We have successfully developed P(NMe)-mediated reductive cyclopropanation, which provides a new, facile, and efficient protocol for the synthesis of cyclopropyl carbocyclic nucleosides, wherein the cyclopropyl group is linked to the nucleobase via a methylene group. This method utilizes safe, commercially available α-keto esters for metal-free cyclopropanation under mild conditions with high yield and diastereoselectivity, demonstrating broad applicability and practical utility in carbocyclic nucleoside synthesis.
View Article and Find Full Text PDF