CAS: 1143-70-0; 3,8-Dihydroxy-6H-Benzo[c]Chromen-6-One

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间甲氧基苯甲醇置于potassium Permanganate,水,氢溴酸,溴,溶剂黄146,Sodium Hydroxide体系中,用 水 用作溶剂,化学反应 13.33H,反应生成尿石素a
参考文献:尿石素作为连接支架的鞣花酸和香豆素类似物:强大的蛋白激酶ck2抑制剂的设计.
标题:尿石素作为连接支架的鞣花酸和香豆素类似物:强大的蛋白激酶ck2抑制剂的设计.
摘要:酪蛋白激酶2(ck2)是一种普遍存在的,必不可少的,高度多效的蛋白激酶.其异常高的本构活性被怀疑是其在瘤形成和其他相关疾病中的致病潜能的基础.以前,使用不同的计算机筛选方法,我们小组确定了两种有效的选择性ck2抑制剂:鞣花酸,天然存在的鞣酸衍生物(k I = 20 N M)和3,8-Dibromo‐7‐hydroxy‐4-甲基铬n-2-One(dbc,K I = 60 N M).比较鞣花酸和dbc的晶体学结合模式,采用x射线结构驱动的合并方法设计了具有改善的靶标亲和力的新型ck2抑制剂.尿石素部分被提议作为两种已知的ck2抑制剂鞣花酸和dbc之间的可能搭桥支架.优化尿石素a作为桥联部分导致鉴定出4-溴-3,8-二羟基苯并[c] Chromen-6-One作为新型,有效和选择性的ck2抑制剂,其k I值为7 N M对抗蛋白激酶,与两个亲本片段相比,对靶标的亲和力显着提高.
Doi:10.1002/cmdc.201100338

专利信息

专利号:US-12338224-B2
优先权日:2018-02-27
标 题 :Process-scale synthesis of urolithin A
发明人：SKRANC WOLFGANG; YIANNIKOUROS GEORGE; TROFIMOV ALEXANDER; SHAN ZHIXING; GOSS CHRISTOPHER
权利人:AMAZENTIS SA
摘要:Methods for preparing a salt of urolithin A and, in turn, urolithin A. Combining in an alkaline aqueous solution a copper-containing catalyst, 2-bromo-5-hydroxybenzoic acid, and resorcinol produces a salt of urolithin A. Urolithin A has been prepared by protonating a salt of the compound.

专利号:US-9573922-B2
优先权日:2013-12-23
标题:Process-scale synthesis of urolithins
发明人：RINSCH CHRISTOPHER; MUELLER ROLAND; SKRANC WOLFGANG
权利人:AMAZENTIS SA
摘要:Disclosed is a method of preparing a urolithin, or an intermediate or analog thereof, having a dibenzo[b,d]pyran-6-one core. The method is especially advantageous for the large-scale preparation of urolithins or intermediates or analogs thereof. The method may optionally include the preparation of a urolithin, or an intermediate or analog thereof, as a pharmaceutically acceptable salt.

专利号:WO-2023198486-A1
优先权日:2022-04-13
标题 :Urolithin butyrate compounds
发明人：BONRATH WERNER; IMHOF ROMAN; PENG KUN; WU LIUHAI
权利人:DSM IP ASSETS BV
摘要:The present invention relates to new specific Urolithin butyrate compounds and to the synthesis of these specific Urolithin butyrates as well as to new compounds and their use. Butyrate compounds are very useful compounds, either as such or as intermediates in organic synthesis.

专利号:US-2023357176-A1
优先权日:2018-02-27
标题:Process-scale synthesis of urolithin a

专利号:US-11634401-B2
优先权日:2018-02-27
标题 :Process-scale synthesis of urolithin A

专利号:US-10906883-B2
优先权日:2018-02-27
标题:Process-scale synthesis of urolithin A