METHOD OF PREPARATION OF THE DERIVATIVE OF THE 3,4,5,6-TEREAHYDRO-4-HYDROXY-2H-PYRAN-2-ON

摘要

6-Phenyl, phenalkyl- and phenylethenyl-4-hydroxytetrahydropyran-2-ones in the 4- R trans stereoisomeric forms having the structure wherein A is H or methyl; E is a direct bond, -CH2-, -CH2-CH2-, -CH2-CH2-CH2- or -CH=CH-; and R1, R2 and R3 have several meanings, and the corresponding dihydroxy acids in which the lactone ring is hydrolytically opened, and the pharmaceutically acceptable salts of said dihydroxy acids, and the lower alkyl and the phenyl, dimethylamino or acetylamino-substituted lower alkyl esters of said dihydroxy acids; and processes for preparing them. These compounds are potent inhibitors of cholesterol synthesis by the enzyme hydroxymethyl glutaryl coenzyme A reductase.