[EN] 11,13-MODIFIED SAXITOXINS FOR THE TREATMENT OF PAIN<br/>[FR] SAXITOXINES MODIFIÉES 11,13 POUR LE TRAITEMENT DE LA DOULEUR
申请人:SITEONE THERAPEUTICS INC
公开号:WO2020072835A1
公开(公告)日:2020-04-09
Provided herein are compounds, pharmaceutical compositions comprising the compounds, methods of preparing the compounds, and methods of using the compounds and compositions in treating conditions associated with voltage-gated sodium channel function where the compounds are 11,13-modified saxitoxins according to Formula (I): (Formula (I)); where R1, and R2 are as described herein.
作者:Larisa Politanskaya、Nadezhda Troshkova、Evgeny Tretyakov、Chanjuan Xi
DOI:10.1016/j.jfluchem.2019.109371
日期:2019.11
A simple and efficient approach to the synthesis of fluorinated benzofurans including the Sonogashira cross-coupling of o-iodophenols with terminal Ph- and n-Bu-acetylenes, followed by intramolecular cyclization, in good to excellent yields is reported.
Synthesis of polyfluorinated o-hydroxyacetophenones – convenient precursors of 3-benzylidene-2-phenylchroman-4-ones
作者:Larisa Politanskaya、Evgeny Tretyakov、Chanjuan Xi
DOI:10.1016/j.jfluchem.2019.109435
日期:2020.1
to the synthesis of fluorinated o-hydroxyacetophenones in good to excellent yields is reported. We demonstrated a convenient method for replacing the iodine atom in o-iodophenols with MeC(=O)– group through the introduction and subsequent hydrolysis of TIPS–C≡C– moiety by of p-toluenesulfonic acid monohydrate. The resulting compounds may serve as precursors for the synthesis of polyfluorinated 3-ben