PROCEDEU DE OBTINERE A UNOR ACIZI PROPIONICI DE SUBSTITUTIE

摘要

1382996 Biphenyl derivatives BOOTS CO Ltd 7 March 1972 [26 March 1971] 7936/71 Heading C2C Novel biphenyl derivatives of the general formula wherein each of R 1 , R 2 and R 3 is a chlorine, bromine or fluorine atom and Y is COOH, CONH 2 , CH 2 OH or CONHOH, and pharmaceutically acceptable esters, inorganic base addition salts and organic base addition salts of those derivatives wherein Y is COOH and inorganic base addition salts of those derivatives wherein Y is CONHOH, are prepared, e.g. (a) when Y is COOH, by hydrolysis of the corresponding compound in which Z is CONH 2 , an ester-forming group or a 4,4 - dialkyl - 2- oxazolinyl-(2) group; (b) when Y is COOH, by decarboxylation of the corresponding compound in which the -CH(CH 3 )Y group is replaced by a -C(CH 3 )(COOH) 2 group; (c) when Y is COOH, by oxidation of the corresponding compound in which Y is CHO; (d) when Y is esterified COOH, by esterification of the corresponding compound in which Y is COOH; (e) when Y is COHN 2 , by reaction of the corresponding compound in which Y is CO-halogen with ammonia; (f) when Y is CH 2 OH, by reduction of the corresponding compound in which Y is esterified COOH; (g) when Y is CONHOH, by reaction of the corresponding compound in which Y is esterified COOH with hydroxylamine; and (h) when Y is salified COOH, by reaction of the corresponding compound in which Y is COOH with a base. Pharmaceutical compositions having antiinflammatory activity comprise, as active ingredient, a biphenyl drivative of the above general formula or pharmaceutically acceptable ester or salt thereof as defined above, in association with a pharmaceutical excipient, and may be administered orally, rectally, topically or parenterally.