NEW MATERIAL:5a,6,7,8,9,9a-Hexahydrodibenzofuranacetic acids of formula I (R1 is H, methyl; R2 is H, 1W4C alkyl; X is H, 1W6C alkyl, 4W7C cycloalkyl, phenyl; Y is hydroxyl, 1W4C alkoxyl), their derivatives and salts.
EXAMPLE: 5a,6,7,8,9,9a-Hexahydro-2-dibenzofuranacetic acid.
USE: Anti-inflammatory analgesic, which has high pharmaceutical activity, low toxicity and side-effects.
PREPARATION: A compound of formula II (R2, X are the same as those in formula I) is acetylated with acetyl chloride in the presence of a Lewis acid and the product is made to react with sulfur and a secondary amine as morpholine to give the thioacetamide. The thioacetamide is heated under reflux in an aqueous potassium hydroxide or a solvent mix of water and organic solvent to give the objective compound of formula I where R1 is H and Y is hydroxyl.
MIZOGAMI SUSUMU
HANAZUKA MITSUO
MITSUBISHI YUKA YAKUHIN KK