Dearomative C-C bond formation of benzyl phosphates has been developed. In the presence of a palladium/PAr catalyst, benzyl phosphates reacted with allyl borates to generate the allylated product in a dearomative fashion. The resulting dearomatized molecules were successfully derivatized by Simmons-Smith cyclopropanation and oxidation.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/acs.orglett.8b01807 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Retention mechanism on phosphodiester stationary phases in HILIC and purely aqueous mobile phase, Part I: The problem of hold-up volume determination.
J Chromatogr A
February 2025
HUN-REN Molecular Interactions in Separation Science Research Group, Ifjúság útja 6, H-7624 Pécs, Hungary; Department of Analytical and Environmental Chemistry and Szentágothai Research Center, University of Pécs, Ifjúság útja 6, H-7624 Pécs, Hungary; Institute of Bioanalysis, Medical Scool, University of Pécs, Szigeti út, H-7624 Pécs, Hungary. Electronic address:
Non-destructive chromatographic methods were used to determine the hold-up volumes of four self-packed columns containing embedded phosphate groups. The stationary phases are named Diol-P-C10, Diol-P-C18, Diol-P-Benzyl and Diol-P-Chol. The hydrophobicity of organic ligands bound to the phosphate group increases in the benzyl< decyl < octadecyl
Evaluation of Performance and Stability of a Gel-Type Polymer Sorbent for Recovery of Phosphate from Waste Streams.
ACS Appl Polym Mater
December 2024
School of Chemistry and Chemical Engineering, Queen's University, David Keir Building, Stranmillis Road, BT9 5AG Belfast, Northern Ireland, U.K.
Phosphorus (P) fertilizer is an essential component of our food system with the majority of all mined P rock processed to make mineral fertilizers. Globally however P rock stocks are declining-both in quality and quantity-with poor P management creating a linear economic system where P is mined, globally redistributed into products and eventually discharged into the environment leading to eutrophication. To enable establishment of a circular P economy, whereby P can be recovered from waste for its industrial reuse, requires the development of effective P recovery technologies.
View Article and Find Full Text PDFMonodisperse Chemical Oligophosphorylation of Peptides via Protected Oligophosphorimidazolide Reagents.
Angew Chem Int Ed Engl
December 2024
Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP), Robert-Rössle-Str. 10, 13125, Berlin, Germany.
Protein poly- and oligophosphorylation are recently discovered post-translational modifications that remain poorly characterized due to (1) the difficulty of extracting endogenously polyphosphorylated species without degradation and (2) the absence of synthetic and analytical tools to prepare and characterize poly- and oligophosphorylated species in biochemical contexts. Herein, we report a methodology for the selective oligophosphorylation of peptides with monodisperse phosphate chain lengths (P=3-6). A library of oligophosphorimidazolide (oligoP-imidazolide) reagents featuring benzyl and o-nitrophenylethyl protecting groups was synthesized in moderate-to-good yields (65-93 %).
View Article and Find Full Text PDFUnique pharmacological properties of etrasimod among S1P receptor modulators.
FEBS Open Bio
January 2025
Arena Pharmaceuticals, San Diego, CA, USA.
Etrasimod (ADP334) is an oral, once-daily, selective sphingosine 1-phosphate (S1P) receptor modulator for the treatment of moderately to severely active ulcerative colitis and in development for the treatment of immune-mediated inflammatory diseases. Interaction between S1P and its five receptor subtypes (S1P-S1P) plays a role in several physiologic systems, including the cardiovascular and immune systems. Since differences in S1PR binding and downstream intracellular signaling could contribute to distinct profiles of drug efficacy and safety, we directly compared the S1P selectivity profile of etrasimod to three marketed S1PR modulators: fingolimod, ozanimod, and siponimod.
View Article and Find Full Text PDFDevelopment of -alkylated benzimidazole based cubosome hydrogel for topical treatment of burns.
RSC Adv
October 2024
Department of Zoology, Wildlife and Fisheries, University of Agriculture Faisalabad 38040 Pakistan.
Article Synopsis
- The study evaluates the effectiveness of a cubosomal hydrogel, or cubogel, made from alkylated benzimidazole derivatives for treating burn wounds.
- Six benzimidazole derivatives were synthesized and characterized, leading to the creation of nanoparticles called cubosomes, optimized for drug loading and release.
- The developed cubogel demonstrated superior wound healing performance and contraction compared to commercial creams, showing a high entrapment efficiency and sustained drug release without side effects.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!