【摘要】 本文合成了一系列7位拉电子基团取代的氧杂蒽-2-羧酸及氧杂蒽酮-2-羧酸化合物。经大鼠被动皮肤过敏试验(PCA),显示化合物(Ⅷ),(Ⅻ_b)和(Ⅻ_e)有50～60％的抑制率(PO,200mg/kg),(Ⅻ_d)有54％的抑制率(ⅳ,10mg/kg)。 氧杂蒽酮-2-羧酸(Ⅷ)经黄鸣龙还原反应生成(Ⅸ),但收率低,推测副产物2,2′-二羟基二苯基-甲烷(Ⅹ)的生成机理,改变反应条件,从而提高了(Ⅸ)的收率。化合物(Ⅻ_d)的元素分析和质谱均证明其结构为(Ⅻ_d),但核磁共振谱(溶剂为三氟醋酸)出现异常,而与(Ⅻ_d)在醋酐中回流所得产物(Ⅻ_d)的图谱相同。表明(Ⅻ_d)在三氟醋酸中环合、脱水产生了(Ⅻ_d)。更多还原

【Abstract】 In the present paper, a series of xanthene-2-carboxylic acids and xanthone-2-carboxylic acids with electron withdrawing groups on the 7-position had been synthesized.Xanthone-2-carboxylic acid（Ⅷ） was converted to（Ⅸ） by Huang-Minlon reduction. A by-product, 2, 2’-dihydroxy-diphenylmethane（Ⅹ）, was also obtained in this reaction.Elemental analysis and MS of Compound（Ⅻ_d） was consistent with the assigned structure, but its ¹HNMR spectrum in CF₃COOH solution was identical with that of（Ⅻ_e） obtained by refluxing compound（Ⅻ_d） in acetic anhydride. It follows that compound（Ⅻ_e） was formed through cyclization and dehydration of compound（Ⅻ_d） in CF₃COOH.The results of passive cutaneous anaphylaxis（PCA） assay in rats showed that compound（Ⅷ）, （Ⅻ_b） and（Ⅻ_e） have 50～60% protective effect（po, 200mg/kg） and（Ⅻ_d） 54%（ⅳ, 10 mg/kg）.更多还原