65136-52-9Relevant academic research and scientific papers
Ni-Catalyzed Carboxylation of C(sp2)-S Bonds with CO2: Evidence for the Multifaceted Role of Zn
Yanagi, Tomoyuki,Somerville, Rosie J.,Nogi, Keisuke,Martin, Ruben,Yorimitsu, Hideki
, p. 2117 - 2123 (2020/02/28)
Nickel-catalyzed reductive carboxylation reactions of aryl electrophiles typically require the use of metallic reducing agents. At present, the prevailing perception is that these serve as both a source of electrons and as a source of Lewis acids that may aid CO2 insertion into the Ni-C bond. Herein, we provide evidence for the in situ formation of organometallic species from the metallic reductant, a step that has either been ruled out or has been unexplored in catalytic carboxylation reactions with metal powder reductants. Specifically, we demonstrate that Zn(0) acts as a reductant and that Zn(II) generates arylzinc species that might play a role in the C(sp2)-S carboxylation of arylsulfonium salts. Overall, the reductive Ni-catalyzed C(sp2)-S carboxylation reaction proceeds under mild conditions in a non-amide solvent, displays a wide substrate scope, and can be applied to the formal para C-H carboxylation of arenes.
Discovery of novel benzofuran-based compounds with neuroprotective and immunomodulatory properties for Alzheimer's disease treatment
Montanari, Serena,Mahmoud, Ali Mokhtar,Pruccoli, Letizia,Rabbito, Alessandro,Naldi, Marina,Petralla, Sabrina,Moraleda, Ignacio,Bartolini, Manuela,Monti, Barbara,Iriepa, Isabel,Belluti, Federica,Gobbi, Silvia,Di Marzo, Vincenzo,Bisi, Alessandra,Tarozzi, Andrea,Ligresti, Alessia,Rampa, Angela
, p. 243 - 258 (2019/06/14)
To address the multifactorial nature of Alzheimer's Disease (AD), a multi-target-directed ligand approach was herein developed. As a follow-up of our previous studies, a small library of newly designed 2-arylbenzofuran derivatives was evaluated towards ch
Preparation and applications of phenylquinolinone-based and flavone-based derivative
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Paragraph 0023; 0044; 0045; 0046, (2019/01/10)
The present invention relates to a phenylquinolinone-based and flavone-based derivative and a preparation method thereof, wherein the derivative is a histamine H3 receptor antagonist, can protect andrestore the normal function of central nervous system, e
Synthesis of (aryloxy)alkylamines. 1. Novel antisecretory agents with H+K+-ATPase inhibitory activity
Sanfilippo,Urbanski,Press,Hajos,Shriver,Scott
, p. 1778 - 1785 (2007/10/02)
A series of heterocyclic (aryloxy)alkylamines of structures II and III were prepared and found to possess gastric antisecretory activity. Of the variety of substituted thiazoles, benzoxazoles, and benzothiazoles prepared, thiazole 18, benzoxazole 32, and benzothiazole 47 exhibited gastric antisecretory potency comparable to that of ranitidine in vivo in the pylorous ligated rat model. In an isolated rabbit parietal system, the series of thiazoles, benzoxazoles, and benzothiazoles also demonstrated similar potency to that of ranitidine toward the inhibition of both histamine-stimulated and dcAMP-stimulated uptake of amino[14C]pyrine. These compounds inhibited the H+K+-sensitive ATPase enzyme in isolated gastric microsomes. A direct correlation existed between inhibition of 14C uptake, in vivo antisecretory activity, and inhibition of the H+K+-ATPase enzyme. The more potent antisecretory compounds 18, 32 and 47 were also the more potent enzyme inhibitors. These data suggest that the mechanism responsible for the observed in vitro and in vivo gastric antisecretory activity, in these series of compounds, is a consequence of the inhibition of the H+K+-sensitive ATPase enzyme.
