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    • 21. 发明授权
    • KMST isoeugenol derivatives and pharmaceutical activity
    • KMST异丁香酚衍生物和药物活性
    • US06887878B2
    • 2005-05-03
    • US10608073
    • 2003-06-30
    • Ing-Jun Chen
    • Ing-Jun Chen
    • A61K31/495C07D295/088C07D241/04
    • C07D295/088A61K31/495
    • A compound having the following formula I: where R1 is an alkyl group or an alkenyl group, X represents R2 is selected from the group consisting of a halogen (o, m, p) group such as F, Cl, Br or I, —NH2, —NO2 and a hydrogen group, R3 is a hydrogen group or OH. The compound has pharmacologically α2-adrenergic/5-HT2A antagonist activity, 5-HT re-uptake activity, and anti-oxidant activity. The compound is produced by preparing 4-epoxy isoeugenol, mixing piperazine dissolved in methanol with the 4-epoxy isoeugenol to reflux at 100° C. for approximately 2 to approximately 6 hours, removing the methanol, passing the mixture through a silica gel column chromatography after the removing step, eluting the passed mixture with n-hexane and ethyl acetate, drying the eluted mixture, and crystallizing the dried mixture with methanol.
    • 具有下式I的化合物:其中R 1是烷基或烯基,X表示R 2选自卤素(o, m,p)基团,例如F,Cl,Br或I,-NH 2,-NO 2,和氢基,R 3, 是氢基或OH。 该化合物具有药理学上的α2 - 肾上腺素能/ 5-HT 2A拮抗剂活性,5-HT再摄取活性和抗氧化活性。 该化合物通过制备4-环氧异丁子香酚,将溶于甲醇的哌嗪与4-环氧异丁子香酚混合,在100℃下回流约2至约6小时,除去甲醇,使混合物通过硅胶柱色谱法 在去除步骤后,用正己烷和乙酸乙酯洗脱经过的混合物,干燥洗脱的混合物,并用甲醇使干燥的混合物结晶。