Synthesis of Acetylene Derivatives of Lappaconitine

摘要

Aconitane-type diterpene alkaloids produced by Aconitum and Delphinium plants have proved themselves as cardioactive and psychoactive agents.Lappaconitine(I),used as an antiarrhythmic drug in the hydrobromide form,is among especially promising compounds of this class.Modification of the lappaconitine molecule has increased the antiarrhythmic activity.This communication describes the synthesis of compounds of a new group,namely,acetylene derivatives of diterpene alkaloids.The goals are,first,to follow the influence of acetylenic fragments on the basic antiarrhythmic activity of the alkaloid and,second,to make an attempt to bring diterpene alkaloid derivatives into the group of antitumor drugs.