2-羧基色酮的7-取代衍生物的合成

SYNTHESIS OF 7-SUBSTITUTED CHROM-4-ONE-2-CARBOXYLIC ACID DERIVATIVES

摘要: 本文报道了2-羧基色酮的7-取代衍生物Ⅰ_1～10和Ⅱ_1～8的合成,以Ⅳ为原料与相应的氯代物反应,可得相应的Ⅰ_1～10和Ⅱ_1～20以Ⅰ₆为原料与各种不同胺类反应则可得Ⅱ_3～80 Ⅰ₆和Ⅱ₁具有类似色甘酸钠(DSCG)对被动皮肤过敏(PCA)的保获作用,Ⅰ₉具有较强的体外抑制血小板聚集的作用。

Abstract: A series of 7-substituted chrom-4-one-2,carboxylic acid derivatives Ⅰ_1～10 and 11_1～8 were prepared. Ⅰ_1～10 and 11_1～2 were. obtained from Ⅳ with appropriate chlorides. Ⅱ_3～8 were obtained from the reactions of Ⅰ₅ with amines. Ⅰ₆ and 11₁ showed similar antiallergic activities against passive cutaneous anaphylaxis (PCA) in the rat as compared with DSCG. Ⅰ₉ exhibited a strong anticoagulative activity in vitro.