Paper
Derivatives of 1,2,3,3-tetramethyl-2-azabicyclo[2,2,2]octan-5-trans-ol with antiarrhythmic and other activities. V.
Published 1980 ยท M. Longobardi, F. Bondavalli, P. Schenone
Il Farmaco; edizione scientifica
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Abstract
A series of N,N-dialkyl 5-trans-carbamoyloxy-1,2,3,3-tetramethyl-2-azabicyclo [2,2,2]octanes was prepared by reaction of 1,2,3,3-tetramethyl-2-azabicyclo [2,2,2]octan-5-trans-ol with phosgene, followed by aminolysis of the resulting chlorocarbonate with aliphatic secondary amines. 5-Chloro-1,2,3,3-tetramethyl-2-azabicyclo [2,2,2] octane (cis/trans mixture) was isolated as by-product of the reaction. A number of urethanes showed antiarrhythmic activity in guinea pigs and mice, as well as surface anesthesia in rabbits and infiltration anesthesia in mice, superior or similar to lidocaine. The circulatory, cardiac and respiratory effects in dogs and hens are also described.
The urethane derivatives of 1,2,3,3-tetramethyl-2-azabicyclo[2,2,2]octan-5-trans-ol show antiarrhythmic activity, superior anesthesia properties in rabbits and mice, and circulatory, cardiac, and respiratory effects in dogs and hens
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