【摘要】 本文合成了14个1,3-二羟基氧杂蒽酮衍生物(Ⅱ～Ⅴ,Ⅷ,Ⅸ)。1,3-二羟基氧杂蒽酮与环氧氯丙烷在哌啶存在下反应,产生化合物(Ⅲ)及(Ⅳ)。(Ⅳ)与胺反应可得化合物(Ⅴ)。大鼠被动皮肤过敏试验(PCA)表明化合物(Ⅱ_c)有63％的保护作用(5 mg/kg静脉注射)。更多还原

【Abstract】 In the present paper, fourteen derivatives (Ⅱ～Ⅴ, Ⅷ, Ⅸ) of 1,3-dihydroxyxanthone have been synthesized. Compound Ⅱ was obtained by condensation of 1,3-dihydroxyxanthone with the corresponding halides in the presence of base Compounds Ⅲ and Ⅳ were prepared by treating 1,3-dihydroxyxanthone with epichlorohydrin in the presence of piperidine. Amination of Ⅳ gave compound Ⅴ. Passive cutaneous anaphylaxis (PCA) assay in rats showed that compound Ⅱ_c gave 63% protective effect (5 mg/kg iv). In order to facilitate the introduction of electron-withdrawing substituents, unsuccessful attempts have been made to remove the ketonic group of Ⅰ andⅧ_b by zinc amalgam-HCl reduction or of Ⅸ. by Huang Min lon reaction, the latter suffering demethylation under drastic alkaline conditions.更多还原