具有局部麻醉活性的3 - 二烷基氨基 - 4,7,7 - 三甲基 - N - 苯基双环[2.2.1]庚 - 2 - 烯 - 2 - 亚氨基硫代羧酸的ω - 二烷基氨基烷基酯
omega-Dialkylaminoalkyl esters of 3-dialkylamino-4,7,7-trimethyl-N-phenylbicyclo[2.2.1] hept-2-ene-2-iminothiolic acids with local anesthetic activity.
作者信息
Ranise A, Bondavalli F, Bruno O, Schenone P, Cenicola M L, Donnoli D, Lampa E, Rossi F
机构信息
Istituto di Scienze Farmaceutiche dell'Università, Genova, Italy.
出版信息
Farmaco. 1991 Sep;46(9):1033-41.
A series of omega-dialkylaminoalkyl esters of 3-dialkylamino-4,7,7-trimethyl-N-phenylbicyclo[2.2.1]hept-2-ene-2- iminothiolic acids 3 was prepared by reaction of 4,7,7-trimethyl-3-(dimethylamino or 1-piperidinyl)-N-phenylbicyclo[2.2.1] hept-2-ene-2-thiocarboxamides with a number of omega-chloroalkyldialkylamines in the presence of sodium hydride in DMF or benzene solution. Some esters 3 showed an appreciable local anesthetic activity in mice.
通过使4,7,7-三甲基-3-(二甲氨基或1-哌啶基)-N-苯基双环[2.2.1]庚-2-烯-2-硫代甲酰胺与多种ω-氯代烷基二烷基胺在氢化钠存在下于DMF或苯溶液中反应，制备了一系列3-二烷基氨基-4,7,7-三甲基-N-苯基双环[2.2.1]庚-2-烯-2-亚氨基硫代羧酸的ω-二烷基氨基烷基酯3。一些酯3在小鼠中显示出明显的局部麻醉活性。
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