梁晓天, 卢玉华, 葛大伦, 祁建新. 2-羧基色酮-7-丙酮氧衍生物的合成J. 药学学报, 1983, 18(3): 179-184.
引用本文: 梁晓天, 卢玉华, 葛大伦, 祁建新. 2-羧基色酮-7-丙酮氧衍生物的合成J. 药学学报, 1983, 18(3): 179-184.
LIANG Xiao-tian, LU Yu-hua, GE Da-lun , QI Jian-xin, . SYNTHESIS OF 7-ACETONYLOXY-CHROM-4-ONE-2-CARBOXYLIC ACID DERIVATIVESJ. Acta Pharmaceutica Sinica, 1983, 18(3): 179-184.
Citation: LIANG Xiao-tian, LU Yu-hua, GE Da-lun , QI Jian-xin, . SYNTHESIS OF 7-ACETONYLOXY-CHROM-4-ONE-2-CARBOXYLIC ACID DERIVATIVESJ. Acta Pharmaceutica Sinica, 1983, 18(3): 179-184.

2-羧基色酮-7-丙酮氧衍生物的合成

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

  • 摘要: 本文报道了若干7-丙酮氧基色酮-2-羧酸衍生物的合成。Ⅱ和氯代丙酮反应可得Ⅲ,Ⅲ与甲醛及吗啉进行Mannich反应,未得Ⅳ,而得Ⅵ或Ⅶ。此外,还合成了Ⅷ~Ⅺ,此类化合物没有表现出显著的对抗大鼠被动皮肤过敏(PCA)反应的活性。

     

    Abstract: Some 7-acetonyloxy-chrom-4-one-2-carboxylic acid derivatives were prepared. Ⅲ was obtained from Ⅱ with chloroacetone. Reaction of Ⅲ with formaldehyde and morpholine in ethanol or butanol by Mannich reaction provided not the desired compound Ⅳ, but Ⅵ or Ⅶ.Treatment of Ⅲ with appropriate amines provided the corresponding acetonyloxyderivatives Ⅸ, Ⅹ and Ⅺ.None of these compounds showed significant inhibition of passive cutaneous anaphylaixs (PCA) in rats.

     

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