发明名称 ALPHA-HALOAROMATIC AMIDOCARBOXYLIC ACID DERIVATIVE AND ANTIALLERGIC COMPRISING IT
摘要 NEW MATERIAL:A compound shown by the formula I (Y is OH, lower acyloxy, or lower alkoxyl; R<1> is OH, lower acyloxy, or lower alkoxyl; R<2> is H, or lower alkyl; X is halogen). EXAMPLE:2-Bromo-N-( 2-carboxyphenyl )-3-( 3,4-dimethoxyphenyl )-3-hydroxypropionamide. USE:An antiallergic. Showing improved inhibitory activity against 5-lipoxygenase. PREPARATION:An aromatic amidocarboxylic acid derivative shown by the formula II is reacted with a halogenating agent such as bromine, chlorine, etc. to give a compound shown by the formula III (X' is halogen). This compound is then treated with water, methanol, sodium acetate, etc. at room temperature - under heating, a halogen at beta-position is replaced with OH, lower acyloxy, or lower alkoxyl, to give a compound shown by the formula I .
申请公布号 JPS60146856(A) 申请公布日期 1985.08.02
申请号 JP19830249547 申请日期 1983.12.30
申请人 KISSEI YAKUHIN KOGYO KK 发明人 MOMOSE DENICHI
分类号 A61K31/19;A61K31/195;A61K31/215;A61K31/22;A61K31/245;A61P37/08;C07C235/38 主分类号 A61K31/19
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