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Cardiovascular Risk Factor and Atherosclerosis in Rheumatoid Arthritis (RA).
Curr Cardiol Rep
January 2025
Division of Rheumatology, Department of Internal Medicine, Texas Tech Health Sciences Center El Paso, Paul L. Foster School of Medicine, El Paso, TX, USA.
Purpose Of Review: To highlight advancements in managing traditional and rheumatoid arthritis (RA) specific risk factors and the impact of RA treatments on cardiovascular outcomes.
Recent Findings: Advancements in rheumatoid arthritis management have paralleled declining trends in cardiovascular disease risks. Biomarkers like CRP, Lipoprotein(a), Apolipoprotein B 100, and imaging tools such as coronary artery calcium scoring enhance cardiovascular risk stratification, particularly in intermediate-risk RA patients.
A Practical Synthetic Route to Cinnolines: Application to the Design and Synthesis of RSV NNI Inhibitor JNJ-8003 Analogues.
Chemistry
January 2025
Janssen Pharmaceutica NV, chemcial process R&D, BELGIUM.
The manuscript describes the development of an efficient synthetic route to cinnolines, facilitating faster access to JNJ-8003 related Respiratory Syncytial Virus (RSV) non-nucleoside (NNI) inhibitors. Starting from correctly functionalized aryl halides, a Sonogashira reaction followed by SNAr reaction with hydrazine 1,2-dicabroxylate reagents provided dihydrocinnolines directly via in situ 6-endo-dig cyclization. The dihydrocinnolines were conveniently transformed to corresponding cinnolines in one step.
View Article and Find Full Text PDFSynthesis of benzouracils and carbamates from chloroacetamides through carbon-carbon bond cleavage.
Org Biomol Chem
January 2025
Natural and Medical Sciences Research Center, University of Nizwa, P.O. Box 33, Postal Code 616, Birkat Al Mauz, Nizwa, Sultanate of Oman.
This work introduces a mild reaction-condition approach for the direct C-C bond cleavage of amides, resulting in the formation of benzouracil and carbamate structures. This method leverages a C-C bond cleavage strategy that enables nucleophilic addition to the amide carbonyl, involving a reactive spiro intermediate. A diverse range of chloroacetamides were synthesized and utilized as bifunctional starting materials in this transformation.
View Article and Find Full Text PDFTransformative reactions in nitroarene chemistry: C-N bond cleavage, skeletal editing, and N-O bond utilization.
Org 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 PDFOne-Pot Synthesis of 2-Substituted Indoles and 7-Azaindoles Sequential Alkynylation and Cyclization of 2-Iodo--mesylarylamines and Alkynes in the Presence of CuO.
Asian J Org Chem
January 2025
Department of Medicinal Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, New Jersey 08854, USA.
A one-pot process was developed to synthesize in moderate to high yield a series of 2-substituted indoles and 7-azaindoles starting from 2-iodo--mesylarylamines and terminal alkynes in the presence of CuO in DMF at 90-120 °C. Without isolation of any intermediate, our optimized conditions enabled the introduction of ester, phenyl, hydroxymethyl, hydroxyethyl, -Boc-aminomethyl, and methyl at the 2-postion of indoles and 7-azaindoles. The reaction tolerates a variety of substrates containing halogens, or acid- or base-sensitive functional groups without requiring a Pd catalyst, a ligand, or a base.
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