NOVEL BICYCLOOCTANE DERIVATIVE, ITS SALT AND THEIR PREPARATION

摘要

NEW MATERIAL:The compound of formulaI(R<1> and R<2> are H or lower alkyl; X is ethylene or vinylene; Y is O or single bond; Z and Z' are H or OH-protecting group; A is halogen, lower alkyl or phenyl which may be substituted with CF3). EXAMPLE:2beta-[3'beta-Hydroxy-4'-(p-fluorophenoxy)-trans-1'-butenyl]-3 alpha-hydroxy-7beta- (3''-carboxypropoxy)-cis-bicyclo[3,3,0]octane. USE:Remedy for ulcer. It has strong antiulcer activity similar to prostacycline, and nevertheless, has extremely low blood platelet coagulation inhibiting acitivity and hypotensive activity, and is chemically stable. PROCESS:The compound of formulaIcan be prepared by hydrolyzing e.g. the nitrile derivative of formula II in a proper solvent in the presence of a base. The product can be converted if necessary, to another form of the compound of formulaIe.g. by esterifying the carboxylic acid, removing the OH-protecting group, etc.