70298-82-7Relevant articles and documents
Organocatalytic Enantioselective Synthesis of Atropisomeric Aryl-p-Quinones: Platform Molecules for Diversity-Oriented Synthesis of Biaryldiols
Chen, Ye-Hui,Li, Heng-Hui,Li, Shaoyu,Tan, Bin,Xiang, Shao-Hua,Zhang, Xiao
supporting information, p. 11374 - 11378 (2020/05/25)
Presented here is a class of novel axially chiral aryl-p-quinones as platform molecules for the preparation of non-C2 symmetric biaryldiols. Two sets of aryl-p-quinone frameworks were synthesized with remarkable enantiocontrol by means of chiral phosphoric acid catalyzed enantioselective arylation of p-quinones by central-to-axial chirality conversion. These aryl-p-quinones were then used to access a wide spectrum of highly functionalized non-C2 symmetric biaryldiols with excellent retention of the enantiopurity.
Substituted 2-anilines as Potential Inhibitors of H+/K+ ATPase
Adelstein, Gilbert W.,Yen, Chung H.,Haack, Richard A.,Yu, Stella,Gullikson, Gary,et al.
, p. 1215 - 1220 (2007/10/02)
A series of substituted 2-anilines were synthesized as potential inhibitors of the acid secretory enzyme H+/K+ ATPase.Substitutions on the aniline nitrogen atom resulted in potent enzyme inhibition in vitro but weak activity in gastric fistula dogs.Electron-donating substituents on the aniline ring enhanced in vitro and in vivo potency relative to the unubstituted analogue.The potency showed a correlation to the calculated pKa of the aniline nitrogen atom.Substitutions on the aniline and benzimidazole rings did not further enhance potency.Di- and trisubstituted aniline derivatives were potent inhibitors of the enzyme system.The preferred combination of substituents were a methoxy group on the benzimidazole ring and a single alkyl group on the aniline ring.One such compound, 76, was an effective inhibitor of acid secretion in the dog and was selected for further pharmacological study.
