CAS: 520-27-4; 5-Hydroxy-2-(3-Hydroxy-4-Methoxyphenyl)-7-(((2S,3R,4S,5S,6R)-3,4,5-Trihydroxy-6-((((2R,3R,4R,5R,6S)-3,4,5-Trihydroxy-6-Methyltetrahydro-2H-Pyran-2-yl)Oxy)Methyl)Tetrahydro-2H-Pyran-2-yl)Oxy)-4H-Chromen-4-One

上下游产品

CAS号520-26-3 橙皮苷 | CAS号69081-76-1 (2R,3Ξ)-5-aceto... | CAS号480-44-4 金合欢素； 刺槐素 | CAS号5128-44-9 5-羟基-4’,7-二甲氧基黄酮 | CAS号480-36-4 蒙花苷 | CAS号520-34-3 香叶木素

Hesperidin置于吡啶,碘体系中,10.0~170.0 °C,1.0 Mpa 条件下,反应 0.54H,以81.96%的收率获得产物地奥司明
参考文献:黄酮类化合物的连续流微通道合成工艺
标题:黄酮类化合物的连续流微通道合成工艺
摘要:本发明提供了黄酮类化合物的连续流微通道合成工艺.所述工艺以橙皮苷,碘单质为原料,在反应溶剂的存在下,于连续流微通道反应器中反应合成式a所示黄酮类化合物.与传统釜式制备工艺相比,本发明的工艺明显缩短了制备时间,明显提高了原料的转化率和产物的收率;特别是在本发明连续流微通道合成的优选工艺条件下制备地奥司明时,原料橙皮苷转化率高达96.48%,产品地奥司明收率高达81.96%.本发明提供的连续流微通道合成工艺,有利于实现黄酮类化合物的安全,高效,快捷的工业化生产,应用前景广阔.

专利信息

专利号:US-7371775-B2
优先权日:2003-09-04
标题:7-carboxymethyloxy-3′,4′,5-trimethoxy flavone monohydrate, the preparation method and uses thereof
发明人：YOO MOOHI; KIM DONG SUNG; KIM YONG DUCK; KIM WONBAE
权利人:DONG A PHARMACEUTICALS CO LTD
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.