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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)。
In this paper, a series of xylene-substituted xanthene-2-carboxylic acid and xanthone-2-carboxylic acid compounds have been synthesized. The passive cutaneous anaphylaxis test (PCA) showed that the inhibitory rate of compound (Ⅷ), (Ⅻ_b) and (Ⅻ_e) was 50-60% (PO, 200mg / kg) and that of Ⅻ_d was 54% Ⅳ, 10 mg / kg). The xanthone-2-carboxylic acid (Ⅷ) is reduced to form Ⅸ by a Huangminglong reaction, but the yield is low. It is speculated that the formation mechanism of 2,2’-dihydroxydiphenyl-methane (Ⅹ) Conditions, thereby increasing the yield of (IX). The elemental analysis and mass spectrometry of the compound (Ⅻ_d) both showed that the structure was (Ⅻ_d), but the nuclear magnetic resonance spectrum (trifluoroacetic acid as the solvent) was abnormal and the spectrum of the product (Ⅻ_d) refluxed in (Ⅻ_d) in acetic anhydride was the same . It shows that (Ⅻ_d) cyclization in trifluoroacetic acid, dehydration produced (Ⅻ_d).