7205-90-5Relevant articles and documents
Studies on the synthesis, stability and conformation of 2-sulfonyl-oxetane fragments
Morgan,Hollingsworth,Bull
, p. 5265 - 5272 (2015/05/13)
2-(Arylsulfonyl)oxetanes have been prepared as new structural motifs of interest for medicinal chemistry. These are designed to fit within fragment space and be suitable for screening in fragment based drug discovery, as well as being suitable for further elaboration or incorporation into drug-like compounds. The oxetane ring is constructed through an efficient C-C bond forming cyclisation which allows the incorporation of a wide range of aryl-sulfonyl groups. Furthermore, biaryl-containing compounds can be accessed through Suzuki-Miyaura coupling from halogenated derivatives. With a number of oxetane containing fragment compounds available, their pH stability was assessed, indicating good half-life values for mono-substituted aryl sulfonyl oxetanes across the pH range (1 to 10). Solubility and metabolic stability data is also reported. Finally, the conformation of the fragments is assessed computationally, providing an indication of possible binding orientations.
A simple and efficient synthesis of trihalomethyl and dihalonitromethyl aryl sulfones
Borys, Krzysztof M.,Korzynski, MacIej D.,Ochal, Zbigniew
, p. 6606 - 6610,5 (2012/12/12)
A method for the preparation of aryl trihalomethyl sulfones - active biocidal agents - with identical or different halogens is presented. The synthesis is based on the reaction of aryl methyl, aryl halomethyl, or aryl nitromethyl sulfones with sodium hypohalite. The method is simple in implementation, does not necessarily require the use of organic solvents, and selectively affords the products in good to excellent yields. Notably, it allows the preparation of the hitherto unknown phenyl trihalomethyl sulfone with three different halogens: fluorine, chlorine, and bromine.
Synthese et activite biologique de prodrogues de l'acide oxolinique
Loubinoux, B,Colin, JL,Thomas, V
, p. 461 - 467 (2007/10/02)
Synthesis and biological activities of oxolinic acid pro-drugs.Antiseptic phenols, anti-inflammatory acids and polyethyleneglycol moieties have been attached by labile bonds to oxolinic acid giving pro-drugs with anti-bacterial activities.Some of them are more soluble in water, exhibit a more sustained action in the time and give higher plasma and tissue concentrations compared with the free drug.