ALPHA-HALOAROMATIC AMIDOCARBOXYLIC ACID DERIVATIVE AND ANTIALLERGIC COMPRISING IT
NEW MATERIAL:A compound shown by the formula I (Y is OH, lower acyloxy, or lower alkoxyl; R and R are halogen, H, or R and R are bonded to each other to form chemical bond; R is H, lower alkyl; X is halogen). EXAMPLE:2,3-Dibromo-N-(2-carboxyphenyl)-3-(3,4-dimethoxyphenyl)propion amide. USE:An antial...
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Zusammenfassung: | NEW MATERIAL:A compound shown by the formula I (Y is OH, lower acyloxy, or lower alkoxyl; R and R are halogen, H, or R and R are bonded to each other to form chemical bond; R is H, lower alkyl; X is halogen). EXAMPLE:2,3-Dibromo-N-(2-carboxyphenyl)-3-(3,4-dimethoxyphenyl)propion amide. USE:An antiallergic. Showing improved inhibitory activity against 5-lipoxygenase. PREPARATION:An alpha,beta-dihalocarboxylic acid shown by the formula II (R' is halogen) or its reactive derivative is reacted with anthranilic acid shown by the formula III or its ester in a solvent such as methylene chloride, etc. in the presence of a base such as pyridine, etc. at room temperature - under heating, to give a compound shown by the formula I (when R is halogen and R is H). |
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