Ranise A, Bondavalli F, Bruno O, Schenone P, Faillace G, Coluccino A, Filippelli W, Di Sarno A, Marmo E
Istituto di Scienze Farmaceutiche dell'Università Genova, Italy.
Farmaco. 1990 Feb;45(2):187-202.
The synthesis of 3-exo-dialkylamino-(Z)-camphoroximes 7 starting from a mixture of 3-endo- and 3-exo-bromocamphornitrimine, hydroxylamine hydrochloride and excess secondary amine (dimethylamine, pyrrolidine, piperidine or morpholine) is described. Compounds 7 gave a series of omega-dialkylaminoalkyl ethers 9, 10 and 11 by reaction of 7 as sodium salts with omega-chloroalkyldialkylamines in DMF solution. Some of compounds 9, 10, 11 showed an appreciable antiarrhythmic and local anesthetic activity in rats and mice, respectively.
描述了从3-内型-和3-外型-溴樟脑亚胺、盐酸羟胺和过量仲胺(二甲胺、吡咯烷、哌啶或吗啉)的混合物开始合成3-外型-二烷基氨基-(Z)-樟脑肟7的方法。化合物7作为钠盐在DMF溶液中与ω-氯烷基二烷基胺反应,得到了一系列ω-二烷基氨基烷基醚9、10和11。化合物9、10、11中的一些分别在大鼠和小鼠中表现出明显的抗心律失常和局部麻醉活性。