4-Benzoyloxymethyl-2,2-Dimethyl-[1,3]Dioxolane置于sodium Carbonate体系中,用 水 用作溶剂,以76%的收率获得(S)-(+)-1,2-异亚丙基甘油 参考文献:Process For Preparation Of 1,3-Dioxolane-4-Methanol Compounds 标题:Process For Preparation Of 1,3-Dioxolane-4-Methanol Compounds 摘要:一种用经济便捷的方法制备1,3-二氧杂环己烷-4-甲醇化合物的工艺,可以制备出具有高纯度和高产率的外消旋形式或光学活性形式.该工艺包括将醇或羧酸的碱金属或碱土金属盐与卤代甲基-1,3-二氧杂环丁烷反应,该卤代甲基-1,3-二氧杂环丁烷是通过在酸催化剂下将具有式(1)的卤代-1,2-丙二醇缩醛化而制备的,其中x是卤素原子,以进行酯化或醚化,然后水解酯基并氢解醚基以制备具有式(5)的1,3-二氧杂环己烷-4-甲醇化合物,其中r^1和r^2是氢原子,具有1至4个碳原子的烷基或苯基,R^1和r^2还可以与相邻的碳原子形成具有3至6个碳原子的环烷基环.
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-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:US-6818633-B2 优先权日:2001-06-29 标题:Antiviral compounds and methods for synthesis and therapy 发明人:BALZARINI JAN M R; DE CLERCQ ERIK D A; HOLY ANTONIN 权利人:ACAD OF SCIENCE CZECH REPUBLIC; REGA STICHTING 摘要:Novel compounds are provided having formula (I)whereR1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).
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.
参考标题:Synthesis Of New Phospholipids Linked To Steroid-Hormone Derivatives Designed For Two-Dimensional Crystallization Of Proteins 作者:Luc Lebeau,Pierre Oudet,Charles Mioskowski |发布日期:1991.12.11 摘要:The Synthesis Of Phospholipids 1N-3N, Rationally Designed For Two-Dimensional Crystallization Of Progesterone And Estradiol Receptors, Is Reported. The Structure Of These Lipids Provides Them With Essential Properties Such As Fluidity And Stability When Spread Into Monolayers At The Air/h2O Interface, Affinity For The Protein To Be Crystallized, And Accessibility Of The Ligand Under The Lipid Monolayer
合成参考文献
摘要:Riva, R.; Banfi, L.; Basso, A., Science of Synthesis: Multicomponent Reactions, (2013) 1, 339. 摘要:Bertau, M.; Jeromin, G. E., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 160. 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2026). 摘要:de Figueiredo, R. M., Science of Synthesis: Knowledge Updates, (2024) 2, 327. 参考文献:10.1016/j.bmc.2006.05.055 摘要:Stadelmaier A, Figueroa-Perez I, Deininger S, von Aulock S, Hartung T, Schmidt RR. A Staphylococcus aureus lipoteichoic acid (LTA) derived structural variant with two diacylglycerol residues. Bioorg Med Chem. 2006 Sep 15;14(18):6239–54. doi: 10.1016/j.bmc.2006.05.055.