Longobardi M, Schenone P, Bondavalli F
Farmaco Sci. 1979 May;34(5):383-9.
Cyanoethylation of 1,2,3,3-tetramethyl-2-azabicyclo[2.2.2]octan-5-endo-ol, followed by LiAlH4 reduction and reaction with acyl chlorides, gave a series of amides derived from 5-endo-(3-aminopropoxy)-1,2,3,3-tetramethyl-2-azabicyclo[2.2.2]octane. The syntheses of N-methyl, N,N-dimethyl and N,N-dipropargyl derivatives of the afore mentioned amine, as well as of 5-endo-methylcarbamoyloxy- and 5-endo-phenylcarbamoyloxy-1,2,3,3-tetramethyl-2-azabicyclo[2.2.2]octane, are also described. Strong antiarrhythmic and local anesthetic activity was observed in two amides; an urethane showed antiarrhythmic activity only.
1,2,3,3-四甲基-2-氮杂双环[2.2.2]辛烷-5-内型醇经氰乙基化反应，接着用氢化铝锂还原并与酰氯反应，得到了一系列由5-内型-(3-氨基丙氧基)-1,2,3,3-四甲基-2-氮杂双环[2.2.2]辛烷衍生而来的酰胺。还描述了上述胺的N-甲基、N,N-二甲基和N,N-二炔丙基衍生物，以及5-内型甲基氨甲酰氧基-和5-内型苯基氨甲酰氧基-1,2,3,3-四甲基-2-氮杂双环[2.2.2]辛烷的合成。在两种酰胺中观察到了强烈的抗心律失常和局部麻醉活性；一种氨基甲酸乙酯仅显示出抗心律失常活性。
