Correction for 'Synthesis of highly substituted 2-spiropiperidines' by Samuel D. Griggs et al., Org. Biomol. Chem., 2018, DOI: 10.1039/c8ob01272e.
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http://dx.doi.org/10.1039/c8ob90117a | DOI Listing |
Angew Chem Int Ed Engl
January 2025
Leibniz University Hanover: Leibniz Universitat Hannover, Institute for Solid State Physics, GERMANY.
Graphdiyne (GDY) has been considered a promising electrode material for application in electrochemical energy storage. However, studies on GDY featuring an ordered interlayer stacking are lacking, which is supposed to be another effective way to increase lithium binding sites and diffusion pathways. Herein, we synthesized a hydrogen-substituted GDY (HsGDY) with a highly-ordered AA-stacking structure via a facile alcohol-thermal method.
View Article and Find Full Text PDFOrg Biomol Chem
January 2025
Department of Applied Chemistry, Waseda University, 513 Wasedatsurumakicho, Shinjuku, Tokyo 162-0041, Japan.
Nitroarenes are highly versatile building blocks in organic synthesis, playing a pivotal role in various reactions. Common transformations involving nitroarenes include nucleophilic aromatic substitution (SAr) reactions, where the nitro group functions both as a potent electron-withdrawing group that activates the aromatic ring and as a leaving group facilitating the substitution. Additionally, the direct transformation of nitro groups, such as reduction-driven syntheses of amines and carboxylic acids, as well as -substitution SAr reactions, have been extensively explored.
View Article and Find Full Text PDFPNAS Nexus
January 2025
Department of Refractory Viral Diseases, National Center for Global Health and Medicine Research Institute, 1-21-1 Toyama, Shinjuku-ku, Tokyo 162-8655, Japan.
We identified a 5-fluoro-benzothiazole-containing small molecule, TKB272, through fluorine-scanning of the benzothiazole moiety, which more potently inhibits the enzymatic activity of SARS-CoV-2's main protease (M) and more effectively blocks the infectivity and replication of all SARS-CoV-2 strains examined including Omicron variants such as SARS-CoV-2 and SARS-CoV-2 than two M inhibitors: nirmatrelvir and ensitrelvir. Notably, the administration of ritonavir-boosted nirmatrelvir and ensitrelvir causes drug-drug interactions warranting cautions due to their CYP3A4 inhibition, thereby limiting their clinical utility. When orally administered, TKB272 blocked SARS-CoV-2 replication without ritonavir in B6.
View Article and Find Full Text PDFFront Pharmacol
January 2025
Phase I Clinical Trial Site, Nanjing Gaoxin Hospital, Nanjing, Jiangsu, China.
Background: Fluticasone propionate is a synthetic trifluoro-substituted glucocorticoid, a highly selective glucocorticoid receptor agonist. Fluticasone propionate nebuliser suspensions is an inhaled corticosteroid with the low systemic bioavailability which provides a low risk (benefit outcome without the adverse effects that accompany systemically administered corticosteroids), referred as a first-line preventive agent for patients with persistent asthma. China has become one of the countries with the highest asthma mortality rate in the world in the past years.
View Article and Find Full Text PDFChem Sci
December 2024
Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry and Sichuan Province, Sichuan Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University Chengdu 610041 China +86 28 85502609.
As a class of readily available and multifunctional building blocks, the chemistry of 4-alken-2-ynyl carbonates remains to be explored. Presented herein is a palladium-catalysed cascade transformative reaction between 4-alken-2-ynyl carbonates and -functionalised activated alkenes. Achiral 1,1-bisalkyl-4-alken-2-ynyl carbonates undergo highly regioselective propargylic substitution with -hydroxyphenyl-tethered activated alkenes, and an auto-tandem vinylogous addition, unusual central-carbon Tsuji-Trost alkylation, protonation and β-H elimination process is followed to furnish fused and spirocyclic frameworks with high structural complexity.
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