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Enantioselective Synthesis of Isoindolinone by Sequential Palladium-Catalyzed Aza-Heck/Suzuki Coupling Reaction.
Org Lett
December 2024
School of Chemistry & Chemical Engineering, Yangzhou University, Yangzhou, Jiangsu 225002, China.
We present a tandem aza-Heck/Suzuki cross-coupling reaction of -phenyl hydroxamic ethers with readily available arylboronic and alkenyl boronic acids. This protocol is enabled by a palladium catalyst paired with chiral phosphoramidite ligands, particularly under mild reaction conditions, yielding efficient and succinct synthetic routes to chiral isoindolinones with high enantioselectivity. Furthermore, this reaction exhibits excellent functional group compatibility and a rich diversity of subsequent transformations.
View Article and Find Full Text PDFOrganocatalytic Enantioselective Arylation to Access Densely Aryl-Substituted P-Stereogenic Centers.
Org Lett
December 2024
Key Laboratory of Green Chemistry & Technology of Ministry of Education, College of Chemistry, Sichuan University, Chengdu 610064, P. R. China.
Although methods for synthesizing chiral phosphorus scaffolds are available, the potential of this molecular chirality remains largely unexplored. Herein, we present a remote desymmetrization of prochiral biaryl phosphine oxides through an organocatalytic asymmetric arylation. This metal-free approach enables the efficient synthesis of a wide range of densely functionalized P(V)-stereogenic compounds with good to excellent yields and satisfactory enantioselectivities.
View Article and Find Full Text PDFDrug-Coated Balloons for the Treatment of Coronary Artery Disease: A Review.
JAMA Cardiol
December 2024
The Zena and Michael A. Wiener Cardiovascular Institute, Icahn School of Medicine at Mount Sinai, New York, New York.
Importance: Drug-coated balloon (DCB) angioplasty has emerged as an alternative to drug-eluting stent (DES) implantation for percutaneous coronary intervention (PCI) in patients with coronary in-stent restenosis (ISR) as well as de novo coronary artery disease.
Observations: DCBs are balloons coated with antiproliferative agents and excipients, whose aim is to foster favorable vessel healing after appropriate lesion preparation. By providing homogeneous antiproliferative drug delivery in the absence of permanent foreign body implantation, DCBs offer multiple advantages over DES, including preservation of vessel anatomy and function and positive vessel remodeling.
New Inhibitors of β-1,4-Galactosyltransferase I Discovered by Virtual Screening.
ChemMedChem
December 2024
University of Ljubljana, Faculty of Pharmacy, Askerceva cesta 7, 1000, Ljubljana, SLOVENIA.
Seven different enzymes comprise the galactosyltransferases family, of which β-1,4-galactosyltransferase I (β-1,4-GALT1) is the major contributor to galactosylation activity in cells. Since abnormalities in galactosylation are associated with many pathophysiological conditions, β-1,4-GALT1 is an interesting new target for drug discovery and molecular probe design. There are several known β-1,4-GALT1 inhibitors, but most of them suffer from low cell permeability and thus low in vivo activity.
View Article and Find Full Text PDFRepresentation of Women Among Cardiology Grand Rounds Speakers in the United States.
JAMA Cardiol
December 2024
Division of Cardiovascular Medicine, Perelman School of Medicine at the University of Pennsylvania, Philadelphia, Pennsylvania.
Importance: Women are underrepresented in leadership positions in cardiology. Institutional grand rounds (GR) are platforms through which faculty can gain professional exposure and access to career development opportunities. The gender diversity of invited cardiology GR speakers has not been investigated.
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