亚麻酸乙酯置于水,Sodium Hydroxide体系中,用 甲醇 作为反应溶剂,化学反应 24.0H,反应生成 γ-十八碳三烯酸 参考文献:Linolenic Acid-Modified Peg-Pcl Micelles For Curcumin Delivery 标题:Linolenic Acid-Modified Peg-Pcl Micelles For Curcumin Delivery 摘要:In This Study,A Novel Linolenic Acid-Modified Poly(Ethylene Glycol)-B-Poly(Epsilon-Caprolactone) Copolymer Was Prepared Through Radical Addition,Ring-Opening Polymerization,And N-Acylation Reactions. Its Structure Was Characterized By H-1 NMR And Gpc. Micelles Were Developed By Thin-Film Hydration And Used As A Delivery System For Curcumin With High Drug Loading Capacity Of 12.80% And Entrapment Efficiency Of 98.53%. The Water Solubility Of Curcumin Was Increased To 2.05 Mg/ml,Which Was Approximately 1.87 X 10(5) Times Higher Than That Of Free Curcumin. The Micelles Were Spherical Shape With An Average Diameter Of 20.8 +/-0.8 Nm. X-Ray Diffraction And Ft-Ir Studies Suggested That Curcumin Existed In The Polymeric Matrices Under Pi-Pi Conjugation And Hydrogen Bond Interaction With The Copolymer. In Vitro Drug Release Studies Indicated That The Curcumin Release From Linolenic Acid-Modified Copolymer Micelles Met Controlled Release,And Its Release Rate Was Less Than That From The Linolenic Acid-Unmodified Copolymer Micelles. Cytotoxicities Against Hela And A-549Cells Demonstrated That The Additional Pi-Pi Conjugation Could Affect Curcumin'S Anticancer Activity Through Reducing Its Release From Micelles. Hemolysis Test And Intravenous Irritation Test Results Revealed That The Linolenic Acid-Modified Copolymer Was Safe For Intravenous Injection. The Plasma Auc(0-Infinity) And Mrt0-Infinity Of Curcumin-Loaded Linolenic Acid-Conjugated Poly(Ethylene Glycol)-B-Poly(Epsilon-Caprolactone) Copolymer Micelles Were 2.75-And 3.49-Fold Higher Than That Of Control Solution,Respectively. The Clz Was Also Decreased By 2.75-Fold. So,This Linolenic Acid-Modified Copolymer Might Be A Carrier Candidate For Curcumin Delivery. (C) 2014 Elsevier B.V. All Rights Reserved. DOI:10.1016/j.Ijpharm.2014.05.059
专利号:US-8383810-B2 优先权日:2004-12-20 标题:Process for the synthesis of azetidinones 发明人:THIRUVENGADAM TIRUVETTIPURAM K; CHIU JOHN S; FU XIAOYONG; MCALLISTER TIMOTHY L 权利人:MERCK SHARP & DOHME; THIRUVENGADAM TIRUVETTIPURAM K; CHIU JOHN S; FU XIAOYONG; MCALLISTER TIMOTHY L 摘要:A process is provided for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, comprising reacting a β-(substituted-amino)amide, a β-(substituted-amino)acid ester, or a β-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride, wherein a quaternary ammonium moiety of the cyclizing agent is unsubstituted or substituted by one to four groups independently selected from the group consisting of alkyl, arylalkyl and arylalkyl-alkyl.
专利号:US-7109377-B2 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products 发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R 权利人:HARVARD COLLEGE 摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
专利号:US-6123959-A 优先权日:1998-04-24 标题:Aqueous composition comprising active ingredients for the de-pigmentation of the skin 发明人:JONES KENNETH; PADMAPRIYA ABEYSINGHE; TEICHMUELLER ERNST E; BLUME GABRIELE 权利人:UNIVERA PHARM INC; ROVI GMBH 摘要:The present invention discloses aqueous compositions comprising liposomes of phospholipids, and at least one competitive inhibitor of an enzyme for the synthesis of melanin, in combination with at least one non-competitive inhibitor of an enzyme for the synthesis of melanin. The invention also includes the use of the compositions of this invention for the de-pigmentation of skin.
专利号:US-2013053592-A1 优先权日:2011-08-31 标题 :Fatty acids as co-catalysts in preparation of glycerides from ethyl esters 发明人:SAEBO ASGEIR 权利人:SAEBO ASGEIR; PHARMA MARINE AS 摘要:Methods of producing concentrates of omega-3 fatty acid ethyl esters, from an ethyl ester composition comprising use of free fatty acids as co-catalysts for enzymatic synthesis of partial glycerides are provided. In some embodiments, methods of producing concentrates of ethyl-eicosapentanoate and/or ethyl-docosahexanoate from an ethyl ester composition containing the esters comprise a) adding glycerol, an immobilized enzyme catalyst, and a free fatty acid co-catalyst b) allow glyceryl ester synthesis to proceed by adjustment of temperatures, time and vacuum such that a substantial amount of partial glycerides is formed and c) separating an ethyl ester fraction enriched in ethyl eicosanoate and ethyl docosahexanoate from the glyceride mixture.
专利号:US-11583842-B2 优先权日:2019-07-24 标题 :Zwitterionic catalysts for (trans)esterification: application in fluoroindole-derivatives and biodiesel synthesis 发明人:YEUNG YING-YEUNG; LAM YING-PONG; KE ZHIHAI; WANG XINYAN; TAN FEI; NG WING-HIN; TSE YING-LUNG STEVE 权利人:UNIV HONG KONG CHINESE 摘要:An amide/iminium zwitterion catalyst has a catalyst pocket size that promotes transesterification and dehydrative esterification. The amide/iminium zwitterions are easily prepared by reacting aziridines with aminopyridines. The reaction can be applied a wide variety of esterification processes including the large-scale synthesis of biodiesel. The amide/iminium zwitterions allow the avoidance of strongly basic or acidic condition and avoidance of metal contamination in the products. Reactions are carried out at ambient or only modestly elevated temperatures. The amide/iminium zwitterion catalyst is easily recycled and reactions proceed in high to quantitative yields.
专利号:US-9487399-B2 优先权日:2010-08-17 标题 :Method for the synthesis of metallic nano products 发明人:GHANAVI JALALEDIN; MOSTAFAVI MEHRNAZ; GHANAVI ZOHRE 权利人:GHANAVI JALALEDIN; MOSTAFAVI MEHRNAZ; GHANAVI ZOHRE 摘要:The embodiments herein provide a method of synthesis for metallic nano-products such as metallic nano-antennas, metallic nano-rods, metallic nano-wires, metallic nano-prolate spheroids and metallic nano-oblate spheroids using saturated and unsaturated carboxylic acids. The method involves preparing a reaction mixture by mixing a polar protic solvent, a polar aprotic solvent or a non-polar solvent, a saturated fatty acid or an unsaturated fatty acid and a metallic salt. Then a mixture of reducing agents is prepared by mixing a polar protic solvent, a polar aprotic solvent or a non-polar solvent and a saturated fatty acid or an unsaturated fatty acid. The reaction mixture and the mixture of reducing agents are combined and heated solvo-thermally for a pre-determined period of time at a pre-determined temperature.
参考文献:10.1194/jlr.m005058 摘要:Degirolamo C, Kelley KL, Wilson MD, Rudel LL. Dietary n-3 LCPUFA from fish oil but not α-linolenic acid-derived LCPUFA confers atheroprotection in mice. Journal of Lipid Research. 2010 Jul;51(7):1897–905. doi: 10.1194/jlr.m005058. 参考文献:10.1042/bj20091762 摘要:Seo PJ, Kim MJ, Song JS, Kim YS, Kim HJ, Park CM. Proteolytic processing of an Arabidopsis membrane-bound NAC transcription factor is triggered by cold-induced changes in membrane fluidity. Biochem J. 2010 Apr 14;427(3):359–67. doi: 10.1042/bj20091762. 参考文献:10.1186/2047-783x-14-s4-248 摘要:Wilczynska-Kwiatek A, Bargiel-Matusiewicz K, Lapinski L. Asthma, allergy, mood disorders, and nutrition. European Journal of Medical Research. 2009 Dec 07;14(Suppl 4):248. doi: 10.1186/2047-783x-14-s4-248. 参考文献:10.1007/s00425-010-1112-2 摘要:Yamauchi Y, Sugimoto Y. Effect of protein modification by malondialdehyde on the interaction between the oxygen-evolving complex 33 kDa protein and photosystem II core proteins. Planta. 2010 Apr;231(5):1077–88. doi: 10.1007/s00425-010-1112-2. 参考文献:10.1007/s10787-010-0033-9 摘要:Kaithwas G, Majumdar DK. Therapeutic effect of Linum usitatissimum (flaxseed/linseed) fixed oil on acute and chronic arthritic models in albino rats. Inflammopharmacology. 2010 Jun;18(3):127–36. doi: 10.1007/s10787-010-0033-9.