Bondavalli F, Longobardi M, Schenone P
Farmaco Sci. 1975 May;30(5):391-8.
Synthesis of twelve N 1-nicotinoyl and isonicotinoylpyrazoles by reaction of 4,5-tetra-, penta-, hexamethylenepyrazoles, dihydronaphtopyrazole, bornylenepyrazole and cineolylenepyrazole with nicotinoyl and isonicotinoylchloride, is described. The structure of N 1-derivatives of these compounds was ascertained by comparison of N.M.R. spectra with those of 1-nicotinoyl and 1-isonicotinoyl-4,5-pentamethylene-5-hydroxy-2-pyrazoline, obtained by reaction of 2-hydroxymethylenecycloheptanone with nicotinoyl and isonicotinoylhydrazide, respectively. N 1-isonicotinoylbornylenepyrazole shows weak C.N.S. depression, muscle relaxation and anticonvulsant activity.
描述了通过4,5 - 四亚甲基、五亚甲基、六亚甲基吡唑、二氢萘并吡唑、冰片烯基吡唑和桉叶烯基吡唑与烟酰氯和异烟酰氯反应合成十二种N1 - 烟酰基和异烟酰基吡唑的方法。通过将这些化合物的N1 - 衍生物的核磁共振谱与分别由2 - 羟基亚甲基环庚酮与烟酰肼和异烟酰肼反应得到的1 - 烟酰基和1 - 异烟酰基 - 4,5 - 五亚甲基 - 5 - 羟基 - 2 - 吡唑啉的核磁共振谱进行比较，确定了这些化合物的结构。N1 - 异烟酰基冰片烯基吡唑显示出较弱的中枢神经系统抑制、肌肉松弛和抗惊厥活性。
