211518-82-0

Basic information

• Product Name: 4-hydroxy-thiophenyl-methyl-diethylphosphonate sulfone
• Synonyms: 4-hydroxy-thiophenyl-methyl-diethylphosphonate sulfone
• CAS NO: 211518-82-0
• Molecular Weight: 308.292
• Mol File: 211518-82-0.mol

Chemical Properties

• CAS DataBase Reference: 4-hydroxy-thiophenyl-methyl-diethylphosphonate sulfone(CAS DataBase Reference)
• NIST Chemistry Reference: 4-hydroxy-thiophenyl-methyl-diethylphosphonate sulfone(211518-82-0)
• EPA Substance Registry System: 4-hydroxy-thiophenyl-methyl-diethylphosphonate sulfone(211518-82-0)

Safety Data

• Hazardous Substances Data: 211518-82-0(Hazardous Substances Data)

Upstream product

• 3084-40-0 diethyl (1-hydroxymethyl)phosphonate 
• 637-89-8 4-sulfanylphenol 
• 31618-90-3 diethyl (p-toluenesulfonyloxymethane)phosphonate 
• 10419-77-9 diethyl iodomethanephosphonate 

Downstream Products

• 1354894-18-0 N-((S)-1-oxo-3-phenyl-1-(((S,E)-5-phenyl-1-((4-(prop-2-yn-1-yloxy)phenyl)sulfonyl)pent-1-en-3-yl)amino)propan-2-yl)morpholine-4-carboxamide 
• 1354894-27-1 (S,E)-5-phenyl-1-((4-(prop-2-yn-1-yloxy)phenyl)sulfonyl)pent-1-en-3-amine trifluoroacetate 
• 1354894-25-9 (S,E)-tert-butyl (5-phenyl-1-((4-(prop-2-yn-1-yloxy)phenyl)sulfonyl)pent-1-en-3-yl)carbamate 
• 1354894-24-8 diethyl (((4-(prop-2-yn-1-yloxy)phenyl)sulfonyl)methyl)phosphonate 

Relevant articles and documents

NOVEL HALO-(3-(PHENYLSULFONYL)PROP-1-ENYL)PYRIDINE DERIVATIVE AND USE THEREOF

The present invention relates to a novel halo-(3-(phenylsulfonyl)prop-1-enyl)pyridine derivative or a pharmaceutically acceptable salt thereof; a preparation method thereof; and an Nrf2 activator and a pharmaceutical composition for preventing or treating diseases induced by a decrease in Nrf2 activity, both of which comprise the same as an active ingredient.

Optimization of Vinyl Sulfone Derivatives as Potent Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) Activators for Parkinson's Disease Therapy

We previously developed a novel series of vinyl sulfones as nuclear factor erythroid 2-related factor 2 (Nrf2) activators with therapeutic potential for Parkinson's disease (PD). However, the previously developed lead compound (1) exhibited undesirable druglike properties. Here, we optimized vinyl sulfones by introducing nitrogen heterocycles to improve druglike properties. Among the synthesized compounds, 17e was the most promising drug candidate with good druglike properties. Compound 17e showed superior effects on Nrf2 activation in cell-based assays compared to compound 1 (17e: half-maximal effective concentration (EC50) = 346 nM; 1: EC50 = 530 nM). Compound 17e was further confirmed to induce expression of Nrf2-dependent antioxidant enzymes at both mRNA and protein levels. In a 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-induced mouse model of PD, 17e significantly attenuated loss of tyrosine hydroxylase-immunopositive dopaminergic neurons, suppressed microglial activation, and alleviated PD-associated motor dysfunction. Thus, 17e is a novel Nrf2 activator with excellent druglike properties and represents a potential therapeutic candidate for PD.

Solid-phase synthesis of peptide vinyl sulfones as potential inhibitors and activity-based probes of cysteine proteases

(Matrix presented) Peptide vinyl sulfones were prepared from 2-chlorotrityl resin-bound phenolic amino vinyl sulfones in high yield and purity. This method enables the convenient synthesis of peptide vinyl sulfones having different amino acids at the Psu