对溴乙基苯置于正丁基锂,硼酸三甲酯,盐酸体系中,用 四氢呋喃,水 作为反应溶剂,化学反应 4.0H,反应生成 4-乙基苯硼酸 参考文献:A Recyclable Au(I) Catalyst For Selective Homocoupling Of Arylboronic Acids: Significant Enhancement Of Nano-Surface Binding For Stability And Catalytic Activity 标题:A Recyclable Au(I) Catalyst For Selective Homocoupling Of Arylboronic Acids: Significant Enhancement Of Nano-Surface Binding For Stability And Catalytic Activity 摘要:由聚苯乙烯-聚丙烯酸微球(ps-Co-Pmaa)稳定的金纳米颗粒被制备并通过x射线衍射(xrd)和透射电子显微镜(tem)进行了表征.涂覆在微球上的金纳米颗粒对芳基硼酸的自偶联反应在芳基卤化物和芳基硼酸的体系中表现出高度选择性的催化活性.催化剂的x射线光电子能谱(xps)显示大量au(I)络合物附着在金纳米颗粒的表面,这有助于芳基硼酸的选择性自偶联.更重要的是,这种支持的金络合物是一种高度可回收的催化剂.支持的金催化剂可以对苯硼酸反应物循环使用至少6次,而原始络合物对该化合物的催化活性非常低.这种材料的高催化活性归因于:(1) 高表面与体积比,导致更多的活性位点暴露于反应物中;(2) 金纳米颗粒与au(I)络合物之间的强表面结合,增强了这些络合物的稳定性和催化活性. DOI:10.1166/jnn.2010.2409
专利号:US-9243004-B2 优先权日:2011-07-22 标题 :Synthesis of boronic esters and boronic acids using grignard reagents 发明人:CLARY JACOB W; SINGARAM BAKTHAN 权利人:CLARY JACOB W; SINGARAM BAKTHAN; UNIV CALIFORNIA 摘要:Boronic esters and boronic acids are synthesized at ambient temperature in an ethereal solvent by the reaction of Grignard reagents with a boron-containing substrate. The boron-containing substrate may be a boronic ester such as pinacolborane, neopentylglycolborane, or a dialkylaminoborane compound such as diisopropylaminoborane. The Grignard reagents may be pre-formed or generated from an alkyl, alkenyl, aryl, arylalkyl, heteroaryl, vinyl, or allyl halide compound and Mg 0 . When the boron-containing substrate is a boronic ester, the reactions generally proceed at room temperature without added base in about 1 to 3 hours to form a boronic ester compound. When the boron-containing substrate is a dialkylaminoborane compound, the reactions generally proceed to completion at 0° C. in about 1 hour to form a boronic acid compound.
专利号:US-12187735-B2 优先权日:2018-09-17 标 题:Matter of composition, synthesis, formulation and application of FL118 platform positions 7 and 9-derived analogues for treatment of human disease 发明人:LING XIANG; LI QINGYONG; LI FENGZHI 权利人:CANGET BIOTEKPHARMA LLC 摘要:Described herein, are the chemical synthesis, matter of compositions, formulation, function, methods and uses of the FL118 platform Positions 7 and/or 9-derived analogues for treating cancer or other human diseases. Compounds derived from chemical modifications of the FL118 platform are employed alone or in combination with other anti-cancer agents to preclude, eliminate or reverse cancer phenotypes. This invention intends to realize unique personalized cancer treatment (personalized precision medicine) through application of a series of structural relevant individual FL118 platform-derived analogues, which target multiple cellular human disease-relevant proteins and their signaling pathways.
专利号:US-2025092058-A1 优先权日:2018-09-17 标 题 :Matter of composition, synthesis, formulation and application of fl 118 platform positions 7 and 9-derived analogues for treatment of human disease 发明人:LING XIANG; LI QINGYONG; LI FENGZHI 权利人:CANGET BIOTEKPHARMA LLC 摘要:Described herein, are the chemical synthesis, compounds, methods and uses of the fluoroaryl-substituted derivatives at the FL118 position 7, which target multiple cellular human disease-relevant proteins and their signaling pathways.
专利号:US-12150934-B2 优先权日:2016-11-30 标 题 :Methods of using substituted pyrazole and pyrazole compounds and for treatment of hyperproliferative diseases 发明人:SIDDIQUI ARSHAD M; CIBLAT STEPHANE; CONSTANTINEAU-FORGET LEA; GRAND-MAITRE CHANTAL; GUO XIANGYU; SRIVASTAVA SANJAY; SHIPPS GERALD W; COOPER ALAN B; OZA VIBHA; KOSTURA MATTHEW W; LUTHER MICHAEL; LEVINE JEDD 权利人:BANTAM PHARMACEUTICAL LLC 摘要:Disclosed are methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for use and uses in medicaments. In certain embodiments, the methods, uses and compounds are provided with reference to compounds of the structural formula (I), in which X1, X2, Z1, Z2, the ring system denoted by “aâ€?, R1, L1, L2, Q, L3, R3, L4, R4, L5, and R5 are as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene.
专利号:US-7781470-B2 优先权日:1999-09-13 标题:Aminodicarboxylic acid derivatives having pharmaceutical properties 发明人:ALONSO-ALIJA CRISTINA; HEIL MARKUS; FLUBACHER DIETMAR; NAAB PAUL; PERNERSTORFER JOSEF; STASCH JOHANNES-PETER; WUNDER FRANK; DEMBOWSKY KLAUS; PERZBORN ELIZABETH; STAHL ELKE 权利人:BAYER SCHERING PHARMA AG 摘要:The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, n nwherein the several variable groups are as defined in the specification and claims. Processes for making these materials, and methods for using them in the synthesis of compounds for treatment of cardiovascular disorders and fibrotic disorders are also disclosed.
专利号:US-2015119580-A1 优先权日:2011-07-22 标 题 :Synthesis of boronic esters and boronic acids using grignard reagents
[参考文献]: Daniel P O'Connell, Et Al. Design And Synthesis Of Boronic Acid Inhibitors Of Endothelial Lipase. Bioorg Med Chem Lett. 2012 Feb 1;22(3):1397-401.
合成参考文献
摘要:Schatz, J.; Seler, M., Science of Synthesis Knowledge Updates, (2011) 2, 401. 摘要:Chetcuti, M. J., Science of Synthesis: N-Heterocyclic Carbenes in Catalytic Organic Synthesis, (2016) 1, 113. 摘要:Xiao, X., Science of Synthesis: Knowledge Updates, (2023) 2, 161.