CAS: 3602-54-8; 2',4'-Dihydroxy-6'-Methoxyacetophenone

上下游产品

2,4,6-trihydroxyacetophenone 1-(2,4,6-trimethoxyphenyl)ethanone 2-hydroxy-4,6-dimethoxyacetophenone dimethyl sulfate 2,4-dihydroxy-6-methoxy-3-aldehydoacetophenone 2-Ethyl-phloroglucin-1-monomethylether 2-O-methyl-4-2',3',4',6'-tetra-O-acetyl-β-D-glucopyranosylphloroacetophenone 4,6-dihydroxy-2-methoxy-5-diphenylmethylacetophenone

📜2,4,6-三羟基苯乙酮一水合物置于三氯化铝,Potassium Carbonate体系中,用 氯苯,丙酮 用作溶剂,化学反应 4.0H,反应生成2',4'-二羟基-6'-甲氧基苯乙酮
参考文献:The Flavone Hispidulin,A Benzodiazepine Receptor Ligand With Positive Allosteric Properties,Traverses The Blood-Brain Barrier And Exhibits Anticonvulsive Effects
标题:The Flavone Hispidulin,A Benzodiazepine Receptor Ligand With Positive Allosteric Properties,Traverses The Blood-Brain Barrier And Exhibits Anticonvulsive Effects
摘要:飞斯丁(4',5,7-三羟基-6-甲氧基黄酮),作为一种效力强大的苯二氮卓(bzd)受体配体,其功能特性研究被启动,以确定其作为中枢神经系统活性调节剂的潜力.在化学合成后,飞斯丁被研究于非洲爪蟾卵母细胞表达的重组gabaa/bzd受体.50 Nm及以上的浓度刺激了测试受体亚型(α1−3,5,6β2γ2S)的gaba诱导的氯电流,表明其正向变构特性.在α1β2γ2S受体中,10 μm的飞斯丁观测到最大刺激.与地西泮不同,飞斯丁调节了α6β2γ2S-Gabaa受体亚型.当应用于癫痫模型中的易抽搐蒙古沙鼠(meriones Unguiculatus)时,飞斯丁(10 Mg/kg体重/天)和地西泮(2 Mg/kg体重/天)显著减少了治疗7天后出现抽搐的动物数量(治疗组分别为30%和25%,而对照组为80%).通过大鼠原位灌流模型,证实了化学合成的,14C标记的飞斯丁穿过血脑屏障的能力.其摄取速率(kin)为1.14 Ml/min/g,测量值接近地西泮等高穿透化合物的值.使用caco-2细胞进行的实验预测,口服的飞斯丁以完整形式进入循环系统.在30 μm浓度下,黄酮类化合物通过单层细胞未发生降解,这一点通过缺乏葡萄糖醛酸化代谢物得以验证.British Journal Of Pharmacology (2004) 142,811-820. Doi:10.1038/sj.Bjp.0705828
Doi:10.1038/sj.Bjp.0705828

专利信息

专利号:US-9061984-B2
优先权日:2008-08-15
标题 :Compounds related to chalcones and benzothienopyrimidines, their synthesis, and uses to treat diseases
发明人：HAMMOND GERALD B; APONTE JOSE C; GILMAN ROBERT H; SAUVAIN MICHEL HENRI AUGUSTE; VAISBERG ABRAHAM
权利人:HAMMOND GERALD B; APONTE JOSE C; GILMAN ROBERT H; SAUVAIN MICHEL HENRI AUGUSTE; VAISBERG ABRAHAM; UNIV LOUISVILLE RES FOUND; UNIV PERUMA CAYETANO HEREDIA; INST RECH POUR LE DÉVELOPPEMENT; UNIV JOHNS HOPKINS
摘要:Embodiments of the present invention provide compounds (such as Formula (I) compounds, Formula (II) compounds, and various embodiments thereof). Compositions comprising those compounds are also provided. Methods for their preparation are included. Also, uses of the compounds are included, such as administering and treating diseases (e.g., cancer and infections).

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.

专利号:CN-105985306-A
优先权日:2015-02-15
标题 :Total synthesis preparation method of natural product flavonoids