1381968-85-9Relevant academic research and scientific papers
Stereoselective Synthesis and Antiallodynic Activity of 3-Hydroxylated Paroxetines
Chamorro-Arenas, Delfino,Salgado-Moreno, Giovanna,Martinez-Mendieta, Liliana,Quintero, Leticia,Godínez-Chaparro, Beatriz,Sartillo-Piscil, Fernando
, p. 472 - 476 (2021)
The design, stereoselective synthesis and in vivo antiallodynic activity of four novel paroxetine analogs, named 3-hydroxy paroxetines (3HPXs), is reported herein. Among the novel synthesized compounds, three showed an antiallodynic effect, while (R,R)-3HPX was found to be 2.5 times more bioactive than (-)-paroxetine itself in neuropathic rats. Consequently, the current investigation not only discloses a novel promising analgesic drug, but also reveals that functionalization at the C3 position of paroxetine could be as effective as the common functionalization at either C4 or within the sesamol group.
Direct chemical method for preparing 2,3-epoxyamides using sodium chlorite
Fuentes, Lilia,Osorio, Urbano,Quintero, Leticia,Hopfl, Herbert,Vazquez-Cabrera, Nixache,Sartillo-Piscil, Fernando
, p. 5515 - 5524 (2012/08/28)
A direct method for preparing 2,3-epoxyamides from tertiary allylamines via a tandem C-H oxidation/double bond epoxidation using sodium chlorite is reported. Apparently, the reaction course consists of two steps: (i) allylic oxidation of the starting allylamine to corresponding unsaturated allylamide with sodium chlorite followed by (ii) epoxidation of the allylamide to the 2,3-epoxyamide mediated by hypochlorite ion, which is formed in situ by reduction of sodium chlorite. The reaction conditions tolerate the presence of free hydroxyl groups and typical functional groups such as TBS, aryl, alkyl, allyl, acetyl, and benzyl groups; however, when an activated aromatic ring (e.g., sesamol) is present in the substrate, the use of a scavenger is necessary.
