1229622-28-9Relevant academic research and scientific papers
Sequential multicomponent catalytic synthesis of pyrrole-3-carboxaldehydes: Evaluation of antibacterial and antifungal activities along with docking studies
Choudhary, Sachin,Kant, Rajni,Kumar, Indresh,Mir, Nisar A.,Ramaraju, Panduga,Sankaranarayanan, Murugesan,Sharma, Preetika,Singh, Rajnish P.,Singh, Rajpal,Vanaparthi, Satheeshvarma
, p. 16329 - 16339 (2020)
A sequential multicomponent synthesis of highly substituted pyrrole-3-carboxaldehydes has been developed under metal-free conditions. This one-pot protocol involves proline-catalyzed direct chemoselective Mannich reaction-cyclization between 1,4-ketoaldehyde and in situ generated Ar/HetAr-imines followed by aerobic oxidative-aromatization at room temperature. A series of fully substituted pyrrole-3-carboxaldehydes and other diverse fused heterocycles have been synthesized. These compounds were tested for in vitro antibacterial and antifungal activities, and the selected ones display significant activity against the tested bacterial strains with a MIC value of 16 μg mL-1, which is close to that of the standard drug chloramphenicol. The bioactivity outcome was further analyzed using docking studies.
A combined computational and experimental investigation of the oxidative ring-opening of cyclic ethers by oxoammonium cations
Loman, Jacob. J.,Carnaghan, Emma R.,Hamlin, Trevor A.,Ovian, John M.,Kelly, Christopher B.,Mercadante, Michael A.,Leadbeater, Nicholas E.
, p. 3883 - 3888 (2016/05/24)
The propensity of oxoammonium cations to facilitate the oxidative ring-opening of cyclic ethers to their corresponding distal hydroxy ketones is investigated. The reaction has been evaluated using experimental and computational methods to gain deeper insight into trends in reactivity.
Catalytic asymmetric intramolecular homologation of ketones with α-diazoesters: Synthesis of cyclic α-Aryl/Alkyl β-ketoesters
Li, Wei,Tan, Fei,Hao, Xiaoyu,Wang, Gang,Tang, Yu,Liu, Xiaohua,Lin, Lili,Feng, Xiaoming
supporting information, p. 1608 - 1611 (2015/01/30)
A catalytic asymmetric intramolecular homologation of simple ketones with α-diazoesters was firstly accomplished with a chiral N,N′-dioxide-Sc(OTf)3 complex. This method provides an efficient access to chiral cyclic α-aryl/alkyl β-ketoesters containing an all-carbon quaternary stereocenter. Under mild conditions, a variety of aryl- and alkyl-substituted ketone groups reacted with α-diazoester groups smoothly through an intramolecular addition/rearrangement process, producing the β-ketoesters in high yield and enantiomeric excess.
Design, synthesis, and biological evaluation of 3-benzazepin-1-ols as NR2B-selective NMDA receptor antagonists
Tewes, Bastian,Frehland, Bastian,Schepmann, Dirk,Schmidtke, Kai-Uwe,Winckler, Thomas,Wuensch, Bernhard
body text, p. 687 - 695 (2010/12/29)
Cleavage and reconstitution of a bond in the piperidine ring of ifenprodil (1) leads to 7-methoxy-2,3,4,5-tetrahydro-1H-3-benzazepin-1-ols, a novel class of NR2B-selective NMDA receptor antagonists. The secondary amine 7-methoxy-2,3,4,5-tetrahydro-1H-3-be
