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1. 发明申请

WO2005023244A1 7-CARBOXYMETHYLOXY-3', 4', 5-TRIMETHOXY FLAVONE MONOHYDRATE, THE PREPARATION METHOD AND USES THEREOF 审中-公开
标题翻译： 7-羧基甲基-3'，4'，5-三甲氧基四氢呋喃单体，其制备方法及其用途
公开(公告)号：WO2005023244A1
公开(公告)日：2005-03-17
申请号：PCT/KR2004/002247
申请日：2004-09-04
申请人： Dong-A Pharmaceutical Co., Ltd. , YOO, Moohi , KIM, Dong Sung , KIM, Yong Duck , KIM, Wonbae
发明人： YOO, Moohi , KIM, Dong Sung , KIM, Yong Duck , KIM, Wonbae
IPC分类号： A61K31/352
CPC分类号： A61K31/352 , C07D311/30 , Y02P20/55
摘要： The present invention relates to 7-carboxymethyloxy-3’, 4’, 5-trimethoxy flavone.monohydrate which is a non hygroscopic product suitable for the preparation of metered dose of 7-carboxymethyloxy-3’, 4’, 5-trimethoxy flavone having protective activity for gastrointestinal tract including the colon, and a preparation method and uses thereof. 7-carboxymethyloxy-3’, 4’, 5-trimethoxy flavone.monohydrate of the present invention has advantages such as mucus protecting activity for gastrointestinal tract including the colon, convenience for handling and storage under ordinary humidity owing to its non-hygroscopicity, and ability to contain an active compound consistently for the formulation production of a medicine. In addition, the preparation method of 7-carboxymethyloxy-3’, 4’, 5-trimethoxy flavone.monohydrate of the present invention reduces long steps of total synthesis and requires mild conditions for the production of a compound because autoclave condition is not necessary for methylation in this case, and makes mass-production possible without any purification process such as recrystallization or column chromatography.
摘要翻译：本发明涉及7-羧甲氧基-3'，4'，5-三甲氧基黄酮一水合物，它是适用于制备计量剂量的7-羧甲氧基-3'，4'，5-三甲氧基黄酮的非吸湿产品，其具有包括结肠在内的胃肠道的保护活性及其制备方法和用途。本发明的7-羧甲氧基-3'，4'，5-三甲氧基黄酮一水合物具有诸如包括结肠在内的胃肠道的粘液保护活性，由于其不吸湿性而在常湿下容易处理和储存的优点，以及能够一致地含有活性化合物来制备药物。此外，本发明的7-羧甲氧基-3'，4'，5-三甲氧基黄酮一水合物的制备方法减少了总合成的长的步骤，并且由于不需要高压灭菌条件，因此对于化合物的制备需要温和的条件在这种情况下甲基化，并且可以在没有任何纯化方法如重结晶或柱色谱法的情况下批量生产。

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