16642-79-8Relevant articles and documents
A Highly Efficient NHC-Catalyzed Aerobic Oxidation of Aldehydes to Carboxylic Acids
Khatana, Anil Kumar,Singh, Vikram,Gupta, Manoj Kumar,Tiwari, Bhoopendra
, p. 4290 - 4294 (2018/11/23)
An N-heterocyclic carbene (NHC) organocatalytic aerobic oxidation of aldehydes to the corresponding carboxylic acids is explored. Remarkably, this method allows for efficient conversion of different classes of aldehydes including highly challenging electron-rich aryl aldehydes, ortho -substituted aryl aldehydes, various heteroaromatic aldehydes and α,β-unsaturated aldehydes under mild reaction conditions. These substrates, under previously reported NHC-catalyzed methods, are typically unreactive or give poor yields, require high reaction temperatures and reaction times of several days.
Design, synthesis and structure–activity relationship studies of novel free fatty acid receptor 1 agonists bearing amide linker
Yang, Jianyong,Li, Zheng,Li, Huilan,Liu, Chunxia,Wang, Nasi,Shi, Wei,Liao, Chen,Cai, Xingguang,Huang, Wenlong,Qian, Hai
supporting information, p. 2445 - 2450 (2017/04/03)
The free fatty acid receptor 1 (FFA1/GPR40) has attracted extensive attention as a novel antidiabetic target. Aiming to explore the chemical space of FFA1 agonists, a new series of lead compounds with amide linker were designed and synthesized by combining the scaffolds of NIH screened lead compound 1 and GW9508. Among them, the optimal lead compound 17 exhibited a considerable agonistic activity (45.78%) compared to the NIH screened compound 1 (15.32%). During OGTT in normal mice, the compound 17 revealed a significant glucose-lowering effect (?23.7%) at the dose of 50?mg/kg, proximity to the hypoglycemic effect (?27.8%) of Metformin (200?mg/kg). In addition, the compound 17 (100?mg/kg) also exhibited a significant improvement in glucose tolerance with a 29.1% reduction of glucose AUC0–2?h in type 2 diabetic mice. All of these results indicated that compound 17 was considered to be a promising lead structure suitable for further optimization.
Synthesis of tetrahydronaphthalene lignan esters by intramolecular cyclization of ethyl p-azidophenyl-2-phenylalkanoates and evaluation of the growth inhibition of human tumor cell lines
Pinto, Orlando,Sardinha, Jo?o,Vaz, Pedro D.,Piedade, Fátima,Calhorda, Maria J.,Abramovitch, Rudolph,Nazareth, Nair,Pinto, Madalena,Nascimento, Maria S. J.,Rauter, Amélia P.
experimental part, p. 3175 - 3187 (2011/07/30)
Figure Presented. Intramolecular cyclization via nitrenium ion of 2-phenylpentanoic/2-phenylbutanoic acid esters with a terminal p-azidophenyl group gives direct access to tetrahydronaphthalene lignan esters. The p-azidophenyl-substituted butanoate led to
