CAS: 208399-66-0; (4-Methoxy-2-Methylphenyl)Boronic Acid

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CAS号27060-75-9 2-溴-5-甲氧基甲苯 | CAS号5419-55-6 硼酸三异丙酯 | CAS号55171-60-3 2-溴-3,4-二甲氧基苯甲醛 | CAS号121-43-7 硼酸三甲酯 | CAS号4235-08-9 3-methoxybenzo[...

📜2-溴-5-甲氧基甲苯置于正丁基锂,硼酸三甲酯,盐酸体系中,用 四氢呋喃,水 用作溶剂,化学反应生成4-甲氧基-2-甲基苯硼酸
参考文献:基于 7-Thiabicyclo[2.2.1]Hept-2-Ene-7-Oxide 的新型雌激素受体配体的鉴定和构效关系
标题:基于 7-Thiabicyclo[2.2.1]Hept-2-Ene-7-Oxide 的新型雌激素受体配体的鉴定和构效关系
摘要:为了开发具有新结构和活性的雌激素受体 (Er) 配体,我们探索了中心疏水核具有更多三维结构的化合物.与通常在雌激素配体中发现的拓扑结构不同,因此利用了配体结合口袋中未填充的空间.在这里,我们在之前对 7-氧杂双环 [2.2.1] 庚烯核心配体的研究的基础上,通过用亚砜替换氧桥.这些新的 7-Thiabicyclo[2.2.1]Hept-2-Ene-7-氧化物可以通过 3,4-二芳基噻吩与亲二烯体在氧化剂存在下的 Diels-Alder 反应方便地制备,并得到具有内立体化学的环加合物.几种新化合物显示出具有优异 Erα 选择性的高结合亲和力,但与作为转录拮抗剂的氧杂双环化合物不同,大多数硫双环化合物是有效的 Erα 选择性激动剂.建模表明,硫双环化合物活性的增加源于它们稳定活性 Er 构象的内立体化学.此外,与双环核心单元相连的苯基中甲基取代基的布置有助于它们的结合亲和力和亚型选择性.
Doi:10.1021/jm201556R

专利信息

专利号:US-6107508-A
优先权日:1998-04-03
标 题 :Convergent synthesis of α-aryl-β-ketonitriles
发明人：ZHOU JIACHENG; OH LYNETTE MAY; MA PHILIP
权利人:DU PONT PHARM CO
摘要:The present invention relates to processes for the production of alpha -aryl- beta -ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists.

专利号:US-7112679-B2
优先权日:1998-04-03
标题:Convergent synthesis of α-aryl-β-ketonitriles
发明人：ZHOU JIACHENG; OH LYNETTE MAY; MA PHILIP
权利人:BRISTOL MYERS SQUIBB PHARMA CO
摘要:The present invention relates to processes for the production of α-aryl-β-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists.

专利号:US-9085511-B2
优先权日:2011-04-04
标题:Atropisomeric 1,8-bisphenolnapthalenes and their use in enantioselective recognition and asymmetric synthesis
发明人：WOLF CHRISTIAN; GHOSN MARWAN
权利人:WOLF CHRISTIAN; GHOSN MARWAN; UNIV GEORGETOWN
摘要:This invention related to atropisomeric 1,8-bisphenolnaphthalenes and derivatives thereof of the general formula (I): n nwhich are useful in resolution of enantiomers, enantioselective recognition and asymmetric synthesis.

专利号:US-2004171829-A1
优先权日:1998-04-03
标 题:Convergent synthesis of alpha-aryl-beta-ketonitriles

专利号:WO-9951568-A2
优先权日:1998-04-03
标 题 :A CONVERGENT SYNTHESIS OF α-ARYL-β-KETONITRILES

专利号:CN-1296473-A
优先权日:1998-04-03
标题:Pooled Synthesis of α-Aryl-β-Ketonitriles