1303974-56-2Relevant articles and documents
Semi-Industrial Fluorination of β-Keto Esters with SF 4: Safety vs Efficacy
Bugera, Maksym Y.,Khairulin, Andrii R.,Kliukovskyi, Denys V.,Ryabukhin, Sergey V.,Semenov, Sergey V.,Shevchenko, Valerii O.,Tarasenko, Karen V.,Trofymchuk, Serhii A.,Volochnyuk, Dmitriy M.
, p. 565 - 574 (2020)
The possibility of deoxofluorination of β-keto esters using SF 4 was investigated. The scope and limitation of the reaction were determined. The efficient method for the synthesis of β,β-difluorocarboxylic acids was elaborated based on the reaction. The set of mentioned acids, being the perspective building blocks for medicinal chemistry, were synthesized on multigram scale. The safety of SF 4 use was discussed. The described method does not improve upon the safety of using SF 4, but practical recommendations for working with the reagent are proposed. Despite the hazards of using toxic SF 4, a significant increase of efficacy in the synthesis of medicinal-chemistry-relevant building blocks, based on the reaction, in comparison with earlier described approaches is shown.
PYRIDO[3,4-B]PYRAZINE DERIVATIVES AS SYK INHIBITORS
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Page/Page column 76-77, (2012/10/07)
A compound of formula (I) or a salt thereof; which is an inhibitor of spleen tyrosine kinase (Syk) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory disease and/or allergic disorders, and in cancer therapy, specifically heme malignancies, and autoimmune conditions.