D-Glucuronidemethylesterd-葡糖苷酸甲酯置于吡啶,氢溴酸体系中,用 溶剂黄146 用作溶剂,化学反应生成乙酰溴-Alpha-D-葡萄糖酮酸甲基酯 参考文献:Synthesis Of Bromophenyl β-D-Glucuronides: Hydrophilic Precursors Of Lipophilic Standards In The Analysis Of Environmental Polychlorinated Biphenyls 标题:Synthesis Of Bromophenyl β-D-Glucuronides: Hydrophilic Precursors Of Lipophilic Standards In The Analysis Of Environmental Polychlorinated Biphenyls 摘要:一个基于提取技术和仪器核活化分析(inaa)结合的快速pcb筛选协议,需要水溶性溴化内标,该内标易于水解为亲脂性溴化对应物.为此应用合成了溴苯基葡糖醛酸2,3,7.葡糖醛酸2和3分别通过溴化苯基β-D-葡萄糖吡喃醛酸制备,收率分别为81%和54%,而化合物7通过甲基2,3,4-三-O-乙酰-α-D-葡萄糖吡喃酸溴化物(5)与2,4,6-三溴苯酚偶联制备.与β-葡糖苷酶孵育表明,三溴苯基衍生物7是一个优秀的底物,在与酶孵育几秒钟后几乎完全转化为三溴苯酚. Doi:10.1135/cccc20061042
专利号:WO-2014131995-A1 优先权日:2013-02-28 标 题 :Method for the enzymatic synthesis of diosmetin derivatives 发明人:PEDRAGOSA MOREAU SANDRINE; LEFOULON FRANÇOIS 权利人:SERVIER LAB 摘要:A method for the enzymatic synthesis of diosmetin derivatives of formula (III):
专利号:US-2014171631-A1 优先权日:2011-08-09 标题:Synthesis of catechin and epicatechin conjugates 发明人:ACTIS GORETTA LUCAS; VITON FLORIAN; BARON DENIS MARCEL; DIONISI FABIOLA 权利人:ACTIS GORETTA LUCAS; VITON FLORIAN; BARON DENIS MARCEL; DIONISI FABIOLA; NESTEC SA 摘要:The present invention relates generally to catechin and epicatechin conjugates of formula (I). For example, a chemical synthesis process for the preparation of catechin and epi-catechin compounds, in particular of catechin and epi-catechin conjugates is disclosed. A further aspect of the invention pertains to new catechin and epi-catechin conjugate compounds.
专利号:US-5218097-A 优先权日:1988-12-07 标题:Process for the preparation of protected mono-sugar and oligo-sugar halides 发明人:ERNST BEAT 权利人:CIBA GEIGY CORP 摘要:The reaction of protected monosaccharides or oligosaccharides or protected monosaccharide and oligosaccharide derivatives containing an anomeric hydroxyl group with secondary α-haloenamines affords high yields of protected glycosyl halides, which are valuable intermediates for the introduction of sugar groups in the synthesis of oligosaccharides, glycolipids or glycopeptides.
专利号:US-12337038-B2 优先权日:2023-04-18 标 题 :Conjugates comprising cleavable beta-glucuronide-containing linkers 发明人:KHAN AKBAR HUSAIN; MADERNA ANDREAS LOTHAR SEVERINO; LEE MAXIMILLIAN TARO WILLIAM; COCCO MATTIA; DENG BOLIANG; BEADLE JONATHAN DAVID; GALAN COCA ALBANO; PRYYMA ALLA; BARTOLO NICOLE DANIELLE; MASTERSON LUKE; GOUNDRY WILLIAM ROBERT FRASER 权利人:ASTRAZENECA AB 摘要:The specification relates to conjugates comprising a linker of Formula (IA): n nand pharmaceutically acceptable salts thereof. The specification also relates the use of the conjugates for the treatment of diseases such as cancer, and intermediates useful for the synthesis of the conjugates.
专利号:US-2025073339-A1 优先权日:2023-08-15 标 题 :Conjugates comprising cleavable linkers 发明人:BEADLE JONATHAN DAVID; GALAN COCA ALBANO; COCCO MATTIA; GOUNDRY WILLIAM ROBERT FRASER 权利人:ASTRAZENECA AB 摘要:The specification relates to conjugates comprising a linker of Formula (IMA): n n n n n n n n n n and pharmaceutically acceptable salts thereof. The specification also relates the use of the conjugates for the treatment of diseases such as cancer, and intermediates useful for the synthesis of the conjugates.
专利号:US-8592458-B2 优先权日:2005-06-07 标 题 :Alpha7 nicotinic receptor selective ligands 发明人:KEM WILLIAM READE; SOTI FERENC 权利人:KEM WILLIAM READE; SOTI FERENC; UNIV FLORIDA 摘要:The invention relates to the design and synthesis of 3-arylidene-anabaseine compounds that exhibit enhanced selectivity toward alpha7 nicotinic receptors. The compounds are expected to be useful in treating a wide variety of conditions, including neurodegenerative conditions such as Alzheimer's Disease, neurodevelopmental diseases such as schizophrenia, and certain peripherally located inflammations mediated by macrophage infiltration.
[参考文献]: Brian T Ethell, Et Al. Glucuronidation Of Hmr1098 In Human Microsomes: Evidence For The Involvement Of Ugt1A1 In The Formation Of S-Glucuronides. Drug Metab Dispos. 2003 Aug;31(8):1027-34. [参考文献]: John C Quindry, Et Al. Mitochondrial Katp Channel Inhibition Blunts Arrhythmia Protection In Ischemic Exercised Hearts. Am J Physiol Heart Circ Physiol. 2010 Jul;299(1):H175-83.
合成参考文献
摘要:Merino, P., Science of Synthesis, (2007) 29, 739. 摘要:Gunn, S. J.; Warriner, S. L.; White, J. W., Science of Synthesis, (2007) 29, 909. 摘要:Kryczka, B.; Lewkowski, J.; Zawisza, A., Science of Synthesis, (2007) 29, 1023.