NOVEL BICYCLOOOCTANE DERIVATIVE AND ITS PREPARATION

摘要

NEW MATERIAL:Bicyclo-octane derivatives of formula I (R1 is H, lower alkyl; R2 is 3-7C alkenyl, 3-7C alkynyl; X is vinylene, ethylene; Y is protecting group for hydroxyl or H). EXAMPLE:2-beta-( 3'-alpha-Hydroxy-trans-1'-octene-5'-ynyl )-3alpha-hydroxy-7E-( 4-methoxycarbonylbutylidene)-cis-bicyclo[3,3,0]octane. USE:Remedy for arteriosclerosis, heart failure or thrombosis: they have blood platelet coagulation activity comparative or superior to PGI2 and the same level of chemical stability as 9(0)metanoprostacyclin. PREPARATION:The reaction of an aldehyde derivative of formula II with an organometal compound of formula: R2-M [M is MgZ (Z is halogen), Li] is effected in an appropriate solvent, when necessary, the protecting group for hydroxyl is removed, and the esterification of carboxylic acid or hydrolysis of ester is conducted to give the compound of formula I.