Arena F, Manna F, Stein M L, Parente L
Farmaco Sci. 1975 May;30(5):380-90.
By reaction of suitable hydroxamic acids chlorides with beta-ketoesters, we have prepared the ethyl esters of isoxazol-4-carboxylic acids, substituted in the 3- and 5-positions with 4-pyridyl and o-chlorophenyl groups, and some of their esters and amides of pharmaceutical interest. 3-(4-Pyridyl)-5-(o-chlorophenyl)isoxazole was obtained either by decarboxylation of the acid or by oxidation of the syn and anti oximes of 3-(o-chlorophenyl)-1-(4-pyridyl)-2-propen-1-one; from the syn oxime the corresponding isoxazoline was also obtained. Pharmacological screening shows that some of the new compounds have a myolytic activity.
通过使合适的异羟肟酸氯化物与β-酮酯反应，我们制备了在3-和5-位被4-吡啶基和邻氯苯基取代的异恶唑-4-羧酸乙酯，以及它们一些具有药学意义的酯和酰胺。3-(4-吡啶基)-5-(邻氯苯基)异恶唑可通过酸的脱羧反应或3-(邻氯苯基)-1-(4-吡啶基)-2-丙烯-1-酮的顺式和反式肟的氧化反应制得；从顺式肟还可得到相应的异恶唑啉。药理筛选表明一些新化合物具有溶肌活性。
