Provided is a novel aromatic ring compound having a GPR40 agonist activity and a GLP-1 secretagogue action. A compound represented by the formula:
wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity and a GLP-1 secretagogue action, is useful for the prophylaxis or treatment of cancer, obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and affords superior efficacy.
Synthesis of Fluoroalkyl Pyrazoles from In-Situ-Generated C<sub>2</sub>F<sub>5</sub>CHN<sub>2</sub>and Electron-Deficient Alkenes
作者:Pavel K. Mykhailiuk、Aleksandr Yu. Ishchenko、Viatcheslav Stepanenko、Janine Cossy
DOI:10.1002/ejoc.201600947
日期:2016.11
C2F5-substituted pyrazolines were synthesized by [3+2]-cycloaddition between in-situ-generated C2F5CHN2 and electron-deficient alkenes. The addition of DBU led to the elimination of HF to give CF3CHF-substituted pyrazoles. Depending on the structure of the pyrazolines, different products were obtained.
Three-component synthesis of fluorinated pyrazoles from fluoroalkylamines, NaNO<sub>2</sub> and electron-deficient alkynes
作者:Pavel K. Mykhailiuk
DOI:10.1039/c4ob02670e
日期:——
Three-component reaction between RCF2CH2NH2.HCl, NaNO2 and electron-deficient alkynes significantly depends on substituent "R". The reaction gives the fluorinated pyrazoles in high yields when "R" is a fluorine atom or a fluoroalkyl group. With other "R" unexpected products are formed.
Traceless N‐Polyfluoroalkylation of Weakly Nucleophilic Nitrogen Containing Compounds
作者:Laura Santos、Florian Audet、Morgan Donnard、Armen Panossian、Jean-Pierre Vors、David Bernier、Sergii Pazenok、Frederic R. Leroux
DOI:10.1002/chem.202300792
日期:——
the high cost, toxicity or environmental impact of commonly used polyfluoroalkylation reagents. We report the sulfuryl fluoride (SO2F2)-mediated N-polyfluoroalkylation of weakly nucleophilic nitrogencompounds from readily available fluorinated alcohols. This method opens access to a variety of N-polyfluoroalkylated building blocks that are highly valuable for life science applications.
由于常用多氟烷基化试剂的高成本、毒性或环境影响, N-多氟烷基化反应具有挑战性。我们报告了硫酰氟 (SO 2 F 2 ) 介导的弱亲核氮化合物的N -多氟烷基化,这些化合物来自现成的氟化醇。该方法开启了对各种N-多氟烷基化构建块的访问,这些构建块对生命科学应用具有很高的价值。