Etherspaltung, ein metabolischer Nebenweg des Etofenamatabbaus bei Versuchstieren

Abstract

Neben den Hauptabbauwegen des Etofenamats bei Versuchstieren und Menschen (Hydroxylierung, Esterspaltung und Konjugation) wurde in der Etherspaltung ein metabolischer Nebenweg gefunden. Nach peroraler Gabe von Etofenamat konnte bei Hunden 5-Hydroxyflufenaminsaure-P-hydroxyethylester (3) aus Faces isoliert und mittels MS und NMR identifiziert werden. In Milch einer mit Etofenamat peroral behandelten Ziege wurde eine Substanz in Spuren mittels GLC nachgewiesen, deren Retentionszeit dem Flufenaminslure-0-hydroxyethylester (2) entspricht. Ether Cleavage, a Side Route of Etofenamate Metabolism in AnimalsIn addition to the main route of etofenamate metabolism in animals and men (hydroxylation, esterolysis and conjugation) ether cleavage was found to be a metabolic side route. P-Hydroxyethyl-5-hydroxyflufenamate (3) was isolated from faeces of dogs after peroral administration of etofenamate and was identified by mass and NMR spectroscopy. In milk of a goat, which got etofenamate by the oral route, a trace metabolite was detected which in GLC showed a retention time like that of f3-hydroxyethyl flufenamate (2). : R = H

Orthogonal Cu- and Pd-Based Catalyst Systems for the O- and N-Arylation of Aminophenols

“…14–22 They have also been applied as building blocks for the preparation of organic materials 23. We were interested in developing a catalytic system capable of selectively arylating either the nitrogen or the oxygen of the different isomers of aminophenols.…”

“…13 O-or N-arylated aminophenol products constitute a common structural motif in various potentially useful therapeutic agents and/or drug candidates (Figure 1). [14][15][16][17][18][19][20][21][22] They have also been applied as building blocks for the preparation of organic materials. 23 We were interested in developing a catalytic system capable of selectively arylating either the nitrogen or the oxygen of the different isomers of aminophenols.…”