29886-66-6Relevant articles and documents
Effective bimetallic composite catalysts for the synthesis of arylated furans and thiophenes in aqueous media
Bumagin, Nikolay A.,Petkevich, Sergey K.,Kletskov, Alexey V.,Alekseyev, Roman S.,Potkin, Vladimir I.
, (2019/08/12)
[Figure not available: see fulltext.] N-(4,6-Dimethylpyrimidin-2-yl)-5-phenylisoxazole-3-carboxamide was used as a ligand for obtaining bimetallic boron-containing heterogeneous catalysts Pd–Ni(Co)–B–L (Ni(Co):Pd = 9:1). The obtained composites were highl
Palladium-catalyzed dehydrogenative coupling of cyclic enones with thiophenes: A rapid access to β-heteroarylated cyclic enones
Wen, Zhen-Kang,Song, Ting-Ting,Liu, Yu-Fang,Chao, Jian-Bin
supporting information, p. 3668 - 3671 (2018/04/12)
Dehydrogenative coupling of cyclic enones with heteroarenes has been a longstanding challenge because of the competitive ketone dehydrogenation and conjugated addition. Herein, a dehydrogenative coupling reaction of cyclic enones of different sizes with substituted thiophenes to construct β-thienyl cyclic enone compounds through palladium-catalyzed C-H functionalization under mild reaction conditions is reported. Simple substituted thiophenes with different functional groups can be directly introduced into cyclic enones with predominant regioselectivity at the α position of thiophene moieties and excellent functional group tolerance. Further molecular transformations of the coupling products to synthetically useful meta-heteroarylated phenol derivatives have also been demonstrated.
Biarylalkyl Carboxylic Acid Derivatives as Novel Antischistosomal Agents
M?der, Patrick,Blohm, Ariane S.,Quack, Thomas,Lange-Grünweller, Kerstin,Grünweller, Arnold,Hartmann, Roland K.,Grevelding, Christoph G.,Schlitzer, Martin
supporting information, p. 1459 - 1468 (2016/07/16)
Parasitic platyhelminths are responsible for serious infectious diseases, such as schistosomiasis, which affect humans as well as animals across vast regions of the world. The drug arsenal available for the treatment of these diseases is limited; for example, praziquantel is the only drug currently used to treat ≥240 million people each year infected with Schistosoma spp., and there is justified concern about the emergence of drug resistance. In this study, we screened biarylalkyl carboxylic acid derivatives for their antischistosomal activity against S. mansoni. These compounds showed significant influence on egg production, pairing stability, and vitality. Tegumental lesions or gut dilatation was also observed. Substitution of the terminal phenyl residue in the biaryl scaffold with a 3-hydroxy moiety and derivatization of the terminal carboxylic acid scaffold with carboxamides yielded compounds that displayed significant antischistosomal activity at concentrations as low as 10 μm with satisfying cytotoxicity values. The present study provides detailed insight into the structure–activity relationships of biarylalkyl carboxylic acid derivatives and thereby paves the way for a new drug-hit moiety for fighting schistosomiasis.