4,5-O-Isopropylidene-L-Arabinose Di(Ethylthio)Acetal置于lead(Iv) Acetate,Sodium Hydroxide,Sodium Tetrahydroborate体系中,化学反应生成(R)-(-)-甘油醇缩丙酮 参考文献:The Synthesis Of Optically Pure Epoxy-Alkyl β-D-Glucosides And β-Cellobiosides As Active-Site Directed Inhibitors Of Some β-Glucan Hydrolases 标题:The Synthesis Of Optically Pure Epoxy-Alkyl β-D-Glucosides And β-Cellobiosides As Active-Site Directed Inhibitors Of Some β-Glucan Hydrolases 摘要:(2R)-和(2S)-2,3-环氧丙基,(3R)-和(3S)-3,4-环氧丁基和(4S)-4,S-环氧戊基 B-吡喃葡萄糖苷,以及(3R)-和(3S)-3,4-环氧丁基 β-胞二糖苷,的制备方法是将溴化糖基与含有作为异亚丙基缩醛保护的二元醇的手性醇的适当对映体缩合,然后将未掩蔽的二元醇与环氧化物官能团结合.此外,对整个过程进行改进后,只需通过对二元醇进行另一种操作,就可以从醇的一种对映体中获得各种环氧丙基和环氧丁基苷的非对映异构体.最后,通过对适当的 4-羟基丁-2-烯基苷进行 Sharpless 不对称环氧化反应,制备出了高光学纯度的 2,3-环氧-4-羟基丁基 β-D 葡糖苷和 β-纤维二糖苷的前体. Doi:10.1071/ch9901391
专利号:US-10266565-B2 优先权日:2011-04-12 标 题 :Peptide mimetic ligands of polo-like kinase 1 polo box domain and methods of use 发明人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG-EUN 权利人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG EUN; THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES 摘要:Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds.
专利号:US-2025236633-A1 优先权日:2022-03-28 标 题:Synthesis of isomerically pure polyol-based phosphoramidites 发明人:BANASIK BRENT; DIAZ CORRAL JULIAN ANDRES; JACOBS AARON; JUD LUKAS; KUCHELMEISTER HANNES; NBAVI MELUD; PFAFFENEDER TONI; SIMONYIOVA SONA; TABONE JOHN C; THUER WILMA 权利人:ROCHE SEQUENCING SOLUTIONS INC 摘要:The present disclosure relates to a process for the regiochemically and enantiomerically controlled synthesis of phosphoramidite-containing monomers, and to intermediate products of this process. In some embodiments, the phosphoramidite-containing monomers or their precursors are regioisomerically and/or enantiomerically pure and may be polymerized into polymers or copolymers.
专利号:US-6384228-B2 优先权日:1998-05-26 标题 :Method for synthesis of halopyridyl-azacyclopentane derivative and intermediate thereof 发明人:NODE MANABU; NAKAMURA DAISAKU; FUJIWARA TOSHIO; ICHIHASHI SHOGO 权利人:NIHON MEDIPHYSICS CO LTD 摘要:The present invention relates to a method for synthesis of an optically active halopyridyl-azacyclo-pentane derivative and the intermediate thereof which comprises preparing an optically active allene-1,3-dicarboxylic acid ester derivative from an optically active acetonedicarboxylic acid ester derivative and then proceeding through a 7-azabicyclo[2.2.1]heptane derivative to obtain the objective product.
专利号:EP-1413627-A1 优先权日:2002-10-25 标题 :Enzymatic synthesis of (S)-1,2-O-isopropylidene glycerol 发明人:MOLINARI FRANCESCO; GANDOLFI RAFFAELLA 权利人:PRIME EUROP THERAPEUTICALS 摘要:Synthesis (M1) of (S)-1,2-O-isopropylidene glycerol(I), involves enzymatic hydrolysis of a racemic mixture of (R,S)-1,2-O-isopropylidene glycerol acetate (II) catalyzed by Kluyveromyces marxianus or an extract or its enzymatically active preparation, and recovery of R form of unreacted 1,2-O-isopropylidene glycerol acetate (II) and hydrolysis of the ester. Synthesis (M1) of (S)-1,2-O-isopropylidene glycerol(I), involves enzymatic hydrolysis of a racemic mixture of (R,S)-1,2-O-isopropylidene glycerol acetate (II) catalyzed by Kluyveromyces marxianus or an extract or its enzymatically active preparation, and recovery of R form of unreacted 1,2-O-isopropylidene glycerol acetate (II) and hydrolysis of the ester. [Image].
专利号:US-8304409-B2 优先权日:2002-07-03 标 题:Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use 发明人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI 权利人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI; NICOX SA 摘要:The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders.
专利号:US-2015031898-A1 优先权日:2012-03-09 标题 :Process for preparation of prostaglandin f2 alpha analogues 发明人:DAMS IWONA; KUTNER ANDRZEJ; CHODYNSKI MICHAL; KRUPA MALGORZATA; PIETRASZEK ANITA; ZEZULA MARTA; CMOCH PIOTR; KOSINSKA MONIKA 权利人:INST FARMACEUTYCZNY 摘要:A convergent synthesis of the prostaglandin F 2α analogues, travoprost and bimatoprost, was developed employing Julia-Lythgoe olefination of the structurally advanced phenylsulfone with an enantiomerically pure aldehyde ω-chain synthon. The novel convergent strategy allows the synthesis of a whole series of prostaglandin analogues of high purity from a common and structurally advanced prostaglandin intermediate.
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合成参考文献
摘要:Bertau, M.; Jeromin, G. E., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 144. 摘要:Casano, G.; Ouari, O., Science of Synthesis, (2021) , 47.