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发明授权
CN101279993B 3-芳基-8-羟基色原酮-7-O-α-D-呋喃阿拉伯糖苷化合物及其合成方法和用途 失效 - 权利终止

3-芳基-8-羟基色原酮-7-O-α-D-呋喃阿拉伯糖苷化合物及其合成方法和用途
摘要：
本发明提供了一条具有强的α-葡萄糖苷酶I、II抑制活性的3-芳基-8-羟基色原酮-7-O-α-D-呋喃阿拉伯糖苷化合物(A-76202类似物)及其合成方法和用途。该方法主要有以下步骤：(1)7，8-二羟基色原酮的合成；(2)7-羟基的选择性裸露；(3)8-羟基-7-(2，3，5-三-O-乙酰基-α-D-呋喃阿拉伯糖基)色原酮的合成；(4)色原酮苷-3-位的溴代；(5)酰基保护基的脱除；(6)Suzuki偶联反应构建异黄酮B环。本发明所制得的A-76202类似物都具有强烈的α-葡萄糖苷酶I、II抑制活性，在开发治疗糖尿病、肥胖、糖鞘脂溶酶体贮存病、HIV感染和肿瘤等药物方面有很好的应用前景。
摘要（英）：

The invention provides 3-aryl-8-hydroxyl-chromone-7-O-Alpha-D-furan arabinoside compound(A-76202analog)with strong inhibiting activity to Alpha-glucosaccharaseI, II, the synthesis method and application thereof. The method includes the following steps: (1)synthesizing 7,8-dihydroxy chromone;(2)selectively disrobing 7-hydroxyl;(3) synthesizing 8-hydroxyl-7-(2,3,5-tri-O-acetyl-Alpha furan arabinoside) chromone; (4) brominating glycoside-3- of chromone; (5) desorbing the protecting group of acyl; (6) constructing isoflavone B Ring through Suzuki coupled reaction. The A-76202 analog prepared withthe method is of strong inhibiting activity to Alpha-glucosaccharaseI, II and is of promising prospect in the development of the drugs for diabetesm, obesity, glycosphingolipid lysosome storage diseases,HIV infection and tumour.

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