20397-61-9Relevant articles and documents
2-Diethoxyphosphoryl alcanoic acid dianions (lithium α-lithiocarboxylates) IV. A direct route to 2-fluoro-2-alkenoic acids by the Horner synthesis. Application in the field of pyrethroids
Coutrot, Ph.,Grison, C.,Sauvetre, R.
, p. 1 - 8 (1987)
2-Diethoxyphosphoryl-2-fluoroacetic acid was converted into the lithium α lithiocarboxylate dianion by treatment with n-butyllithium in hexane/tetrahydrofuran at -70 deg C.The Horner reaction between this new dianion and carbonyl compounds gave various 2-fluoro-2alkenoic acids.Application of the method to the cis,trans caronaldehyde ethyl esters led to the 2-fluoroethenyl pyrethroid derivatives (Z-cis, E-cis, Z-trans, E-trans).
Fluorine-containing carboxylic acid compound and preparation method thereof
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Paragraph 0038-0048; 0054-0057, (2020/09/09)
The invention provides a fluorine-containing carboxylic acid compound and a preparation method and application thereof. The preparation method comprises the steps that a fluorine-containing olefin compound and CO2 react in a solvent in the presence of a c
Development of the First Two-Pore Domain Potassium Channel TWIK-Related K+ Channel 1-Selective Agonist Possessing in Vivo Antinociceptive Activity
Vivier, Delphine,Soussia, Ismail Ben,Rodrigues, Nuno,Lolignier, Stéphane,Devilliers, Ma?ly,Chatelain, Franck C.,Prival, Laetitia,Chapuy, Eric,Bourdier, Geoffrey,Bennis, Khalil,Lesage, Florian,Eschalier, Alain,Busserolles, Jér?me,Ducki, Sylvie
, p. 1076 - 1088 (2017/02/19)
The TWIK-related K+ channel, TREK-1, has recently emerged as an attractive therapeutic target for the development of a novel class of analgesic drugs, suggesting that activation of TREK-1 could result in pain inhibition. Here, we report the synthesis of a series of substituted acrylic acids (1-54) based on our previous work with caffeate esters. The analogues were evaluated for their ability to modulate TREK-1 channel by electrophysiology and for their in vivo antinociceptive activity (acetic acid-induced writhing and hot plate assays), leading to the identification of a series of novel molecules able to activate TREK-1 and displaying potent antinociceptive activity in vivo. Furyl analogue 36 is the most promising of the series.
