GB1414886A - 2,10-dichloro-12-methyl-12h-dibenzo-d,g 1,3 dioxocine derivatives and a process for the preparation of same - Google Patents

Abstract

1414886 2,10-Dichloro-12-methyl-12H-dibenzo(d,g)(1,3)dioxocines EGYT GYOGYSZERVEGYESZETI GYAR 25 Sept 1973 [18 Dec 1972] 44793/73 Heading C2C Novel 2,10-dichloro-12-methyl-12H-dibenzo- (d,g)(1,3)dioxocines of the general formula wherein R is a hydroxy, C 1-4 alkoxy or C 1-4 alkylamino group, and, when R is a hydroxy group, base addition salts thereof are prepared by reacting 1,1-bis-(2-hydroxy-5-chlorophenyl)- ethane with a compound of the general formula Cl 2 CH-COR in the presence of a base and a polar solvent, followed optionally by one or more of the following steps: (a) esterification of a resulting free acid; (b) salification of a resulting free acid; (c) conversion of a resulting acid or ester into the corresponding C 1-4 alkylamide; (d) hydrolysis of a resulting ester or amide to give the corresponding free acid (or a base addition salt thereof); (e) conversion of a resulting ester into another C 1-4 alkyl ester by metathesis; (f) conversion of a resulting salt to the free acid by treatment with an acid; and (g) separation of a resulting mixture of cis- and trans-isomers into the pure isomers. Pharmaceutical compositions having serum cholesterol, triglyceride and free lipoid reducing and liver-protecting activity comprise, as active ingredient, a 2,10-dichloro-12-methyl-12H-dibenzo(d,g)(1,3)dioxocine of the first general formula above, or, when R is a hydroxy group, a pharmaceutically acceptable base addition salt thereof, together with a carrier, binder and/or auxiliary substance usable in the pharmaceutical industry.