28122-13-6Relevant articles and documents
One-Step Synthesis of [18F]Fluoro-4-(vinylsulfonyl)benzene: A Thiol Reactive Synthon for Selective Radiofluorination of Peptides
Ma, Gaoyuan,McDaniel, James W.,Murphy, Jennifer M.
supporting information, p. 530 - 534 (2021/01/13)
Radiolabeled peptide-based molecular imaging probes exploit the advantages of large biologics and small molecules, providing both exquisite selectivity and favorable pharmacokinetic properties. Here, we report an operationally simple and broadly applicable approach for the 18F-fluorination of unprotected peptides via a new radiosynthon, [18F]fluoro-4-(vinylsulfonyl)benzene. This reagent demonstrates excellent chemoselectivity at the cysteine residue and rapid 18F-labeling of a diverse scope of peptides to generate stable thioether constructs.
Process for producing [2-(arylsulfonyl) ethenyl] benzene derivatives
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, (2008/06/13)
The present invention provides a safer and more efficient process for producing [2-(arylsulfonyl)ethenyl]benzene derivatives of the formula (3): wherein R1, R2, R3 and R4 are the same or different and each independently represent a hydrogen, fluorine, or chlorine atom, a lower alkyl group, or the like, and two adjacent R3 and R4 may bond each other at their terminals to form a ring, which the process is characterized in that a 2-(arylsulfonyl)ethanol of formula (1): wherein R1 and R2 are as defined above, and an acid anhydride are reacted in the presence of a base, and the reaction liquid obtained is supplied to a reaction with an aromatic halide of formula (2): wherein X represents a chlorine, bromine, or iodine atom, and R3 and R4 are the same as defined above, in the presence of a palladium catalyst and a base.
