5Beta-胆烷酸-3Alpha,7Alpha,12Alpha-三醇乙酯置于4-二甲氨基吡啶 氢氧化钾,盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺体系中,用 四氢呋喃,甲醇,水 作为反应溶剂,化学反应 0.24H,反应生成 N-(3Alpha,7Alpha,12Alpha)三羟基-5β-胆甾烷-24-酰基牛黄酸 参考文献:Chemical Modifications Of Bile Acids Under High-Intensity Ultrasound Or Microwave Irradiation 标题:Chemical Modifications Of Bile Acids Under High-Intensity Ultrasound Or Microwave Irradiation 摘要:High-Intensity Ultrasound (Hiu) And Microwave (Mw) Irradiation,Having Emerged As Effective Promoters Of Organic Reactions,Were Exploited For The Synthesis Of Bile Acids Derivatives. Esterification,Amidation,Hydrolysis,Oxidation,And Reduction Were Investigated. Compared To Conventional Methods,Both Techniques Proved Much More Efficient,Increasing Product Yields And Dramatically Cutting Down Reaction Times. Scaled-Up Studies Are Now Under Way. (C) 2004 Elsevier Inc. All Rights Reserved. DOI:10.1016/j.Steroids.2004.09.007
专利号:US-6451543-B1 优先权日:1998-08-31 标题:Lipid matrix-assisted chemical ligation and synthesis of membrane polypeptides 发明人:KOCHENDOERFER GERD G; HUNTER CHRISTIE L; KENT STEPHEN B H; BOTTI PAOLO 权利人:GRYPHON SCIENCES 摘要:The present invention relates to methods and compositions for lipid matrix-assisted chemical ligation and synthesis of membrane polypeptides that are incorporated in a lipid matrix. The invention is exemplified in production of a prefolded membrane polypeptide embedded within a lipid matrix via stepwise chemoselective chemical ligation of unprotected peptide segments, where at least one peptide segment is embedded in a lipid matrix. Any chemoselective reaction chemistry amenable for ligation of unprotected peptide segments can be employed. Suitable lipid matrices include liposomes, micelles, cell membrane patches and optically isotropic cubic lipidic phase matrices. Prefolded synthetic and semi-synthetic membrane polypeptides synthesized according to the methods and compositions of the invention also permit site-specific incorporation of one or more detectable moieties, such as a chromophore, which can be conveniently introduced during synthesis. The methods and compositions of the invention have multiple uses. For example, they can be used to assay ligand binding to membrane polypeptides and domains comprising a receptor, and thus are extremely useful for structure/function studies, drug screening/selection/design, and diagnostics and the like, including high-throughput applications. The methods and compositions of the invention are particularly suited for FRET analyses of previously inaccessible membrane polypeptides.
专利号:WO-2004011474-A1 优先权日:2002-07-31 标题:Universal support media for synthesis of oligomeric compounds 发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K 权利人:ISIS PHARMACEUTICALS INC; GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K 摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotide and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.
专利号:US-7202256-B2 优先权日:2004-04-14 标题:Proline CCI-779, production of and uses therefor, and two-step enzymatic synthesis of proline CCI-779 and CCI-779 发明人:GU JIANXIN; RUPPEN MARK E; RAVEENDRANATH PANOLIL; CHEW WARREN; SHAW CHIA-CHENG 权利人:WYETH CORP 摘要:Methods for the synthesis of CCI-779 and proline-CCI-779 are described, including a method involving lipase-catalyzed acetylation of 42-hydroxy of rapamycin with a vinyl ester of 2,2-bis(hydroxymethyl) propionic acid in an organic solvent followed by deprotection. Also provided are products containing proline-CCI-779 and uses thereof.
专利号:US-6653468-B1 优先权日:2002-07-31 标 题 :Universal support media for synthesis of oligomeric compounds 发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH 权利人:ISIS PHARMACEUTICALS INC 摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.
专利号:US-2006211083-A1 优先权日:2005-01-21 标题:Products and processes for in vitro synthesis of biomolecules 发明人:KATZEN FEDERICO; KUDLICKI WIESLAW; FLETCHER JULIA 权利人:KATZEN FEDERICO; KUDLICKI WIESLAW; FLETCHER JULIA 摘要:Provided herein are products and processes for efficiently synthesizing biomolecules in vitro using cell-free extracts derived from mammalian cells and insect cells. In an embodiment, provided is a process for preparing a cell-free extract from insect cells and mammalian cells that efficiently synthesizes post-translationally modified target proteins (e.g., glycosylated target proteins). In some embodiments, a ribonucleic acid is synthesized in vitro that comprises a cap, a 5′ untranslated region comprising an 18S rRNA binding ribonucleotide sequence, and a target ribonucleotide sequence. It has been determined that such ribonucleic acids result in efficient in vitro synthesis of a target protein using cell-free extracts derived from non-rabbit mammalian cells and insect cells.
专利号:US-9828445-B1 优先权日:2016-12-13 标题:Synthesis of modified chitosan particles for oral insulin delivery 发明人:ATTA AYMAN M; AL-LOHEDAN HAMAD A; EZZAT ABDELRAHMAN O 权利人:UNIV KING SAUD 摘要:Synthesis of modified chitosan particles for oral insulin delivery includes amidation of chitosan with a fatty acid, a modified fatty acid, and/or an amino acid. The amidated chitosan can be grafted with N-isopropylacrylamide (NIPAm) and cross-linked to provide the modified chitosan particles.
参考文献:10.2165/11319380-000000000-00000 摘要:Chatzizisis YS, Koskinas KC, Misirli G, Vaklavas C, Hatzitolios A, Giannoglou GD. Risk factors and drug interactions predisposing to statin-induced myopathy: implications for risk assessment, prevention and treatment. Drug Saf. 2010 Mar 01;33(3):171–87. doi: 10.2165/11319380-000000000-00000. 参考文献:10.1039/c1pp05130j 摘要:Pace TCS, Souza Júnior SP, Zhang HT, Bohne C. Effect of terbium(III) on the binding of aromatic guests with sodium taurocholate aggregates. Photochemical & Photobiological Sciences. 2011 Oct;10(10):1568–77. doi: 10.1039/c1pp05130j. 参考文献:10.1371/journal.pone.0022094 摘要:Trottier J, Białek A, Caron P, Straka RJ, Milkiewicz P, Barbier O. Profiling Circulating and Urinary Bile Acids in Patients with Biliary Obstruction before and after Biliary Stenting. PLoS ONE. 2011 Jul 08;6(7):e22094. doi: 10.1371/journal.pone.0022094. 摘要:Xiping Z, Hua T, Hanqing C, Li C, Binyan Y, Jing M. Effects of Baicalin on inflammatory mediators and pancreatic acinar cell apoptosis in rats with sever acute pancreatitis. J Res Med Sci. 2009 Jan;14(1):19–27.