ALDOL DERIVATIVE AND ITS PREPARATION

摘要

NEW MATERIAL:A 2-exo-formyl-3-endo-hydroxy-7-oxo-cis-bicyclo[3, 3, 0]octane shown by the formula I (C=W is carbonyl or carbonyl-protecting group) and its derivative. EXAMPLE:2-Exo-formyl-3-endo-hydroxy-7, 7-ethylenedioxy-cis-bicyclo[ 3, 3, 0 ]octane. USE:A synthetic intermediate of a related compound of prostaglandin I2 (PGI2), that is, a synthetic intermediate of 6, 9 (0) methanoprostacyclin, which is chemically stabler than PGI2 and has the relaxation action of the artery and the control action of agglutination of blood platelet. PROCESS:An olefin derivative shown by the formula III is subjected to oxidative ring cleavage to give a dialdehyde derivative shown by the formula IV which is subjected to intramolecular aldol ring closure to prepare a compound shown by the formula I, from which the title 6, 9, (0) methanoprostacyclin shown by the formula V is obtained.