专利号:US-5977301-A 优先权日:1992-09-24 标题 :Synthesis of N-substituted oligomers 发明人:ZUCKERMAN RONALD N; KERR JANICE M; KENT STEPHEN B H; MOOS WALTER H; SIMON REYNA J; GOFF DANE A 权利人:CHIRON CORP 摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a resin-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability.
专利号:EP-0671928-B1 优先权日:1992-09-24 标题 :Synthesis of n-substituted oligomers 发明人:ZUCKERMANN RONALD N; KERR JANICE M; KENT STEPHEN BRIAN HENRY; MOOS WALTER H; SIMON REYNA J; GOFF DANE A 权利人:CHIRON CORP 摘要:Poly N-substituted Glycines (poly NSGs), wherein the substituents bear purine or pyrimidine bases (R<9>) every second glycine: In addition, a solid phase method for the synthesis of N-substituted oligomers of more general structures is disclosed.The poly NSGs obtainable by this method can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a resin-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using the automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability.
专利号:US-7241399-B2 优先权日:2000-09-08 标题 :Synthesis of nanoparticles 发明人:HAUBOLD STEPHAN; HAASE MARKUS; RIWOTZKI KARSTEN; WELLER HORST; MEYSSAMY HEIKE; IBARRA FERNANDO 权利人:CT ANGEWANDTE NANOTECH CAN 摘要:Methods for the preparation of inorganic nanoparticles capable of fluorescence, wherein the nanoparticles consist of a host material that comprises at least one dopant. The synthesis of the invention in organic solvents allows to gain a considerably higher yield compared to the prior art synthesis in water. All kinds of objects can advantageously be marked and reliably authenticated by using an automated method on the basis of a characteristic emission. Further, the size distribution of the prepared nanoparticles is nartower which renders a subsequent size-selected separation process superfluous.
专利号:US-5877278-A 优先权日:1992-09-24 标题:Synthesis of N-substituted oligomers 发明人:ZUCKERMANN RONALD N; GOFF DANE A; NG SIMON; SPEAR KERRY; SCOTT BARBARA O; SIGMUND AARON C; GOLDSMITH RICHARD A; MARLOWE CHARLES K; PEI YAZHONG; RICHTER LUTZ; SIMON REYNA 权利人:CHIRON CORP 摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a solid support-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability. Combinatorial libraries of cyclic compounds are disclosed wherein the cyclic compounds are comprised of at least one ring structure derived from cyclization of a peptoid backbone. The diversity of product compounds is generated by the sequential addition of substituted submonomers. The combinatorial library includes 10 or more, preferably 100 or more, and more preferably 1,000 or more distinct and different compounds. The library includes each of the product compounds in retrievable and analyzable amounts and preferably includes at least one biologically active compound. Methods of synthesizing the combinatorial libraries and assay devices produced using the libraries are disclosed as is methodology for screening for and obtaining biologically active cyclic organic compounds.
专利号:US-10731001-B2 优先权日:2018-11-09 标 题 :Method for the recovery of compounds deriving from the synthesis of poly aryl ether ketone polymers 发明人:SCHON STEVEN GABRIEL; GODDARD ANDREW RICHARD; JOUANNEAU JULIEN 权利人:ARKEMA FRANCE 摘要:A method for treating a shear-thinning residue composition deriving from the synthesis of an aryl ether ketone, the residue composition including a liquid fraction and solid residues, the method including the steps of: passing said shear-thinning residue composition through a shear-generating evaporating device, between a rotating part and a stationary part; and recovering a condensed liquid fraction and separately recover concentrated solid residues.
专利号:US-7273933-B1 优先权日:1998-02-26 标 题 :Methods for synthesis of oligonucleotides 发明人:KROTZ ACHIM H; RAVIKUMAR VASULINGA T 权利人:ISIS PHARMACEUTICALS INC 摘要:Improved methods for synthesis of oligonucleotides and other phosphorus-linked oligomers are disclosed. The methods include the use of aromatic solvents, alkyl aromatic solvents, halogenated aromatic solvents, halogenated alkyl aromatic solvents, or aromatic ether solvents to achieve deprotection of protected hydroxyl groups.
[参考文献]: Albert Serrà, Et Al. Green Electrochemical Template Synthesis Of Copt Nanoparticles With Tunable Size, Composition, And Magnetism From Microemulsions Using An Ionic Liquid (Bmimpf6). Acs Nano. 2014 May 27;8(5):4630-9. [参考文献]: Ayman M Saleh, Et Al. Synthesis And Biological Evaluation Of New Pyridone-Annelated Isoindigos As Anti-Proliferative Agents. Molecules. 2014 Aug 25;19(9):13076-92. [参考文献]: Bradley Duncan, Et Al. Hybrid Organic-Inorganic Colloidal Composite 'Sponges' Via Internal Crosslinking. Small. 2015 Mar 18;11(11):1302-9. [参考文献]: Bruno F B Silva, Et Al. Nematic Director Reorientation At Solid And Liquid Interfaces Under Flow: Saxs Studies In A Microfluidic Device. Langmuir. 2015 Apr 14;31(14):4361-71. [参考文献]: Do Gyun Lee, Et Al. Biodegradation Of Triclosan By A Wastewater Microorganism. Water Res. 2012 Sep 1;46(13):4226-34.
合成参考文献
参考文献:10.1007/s00216-010-3496-z 摘要:Saraji M, Marzban M. Determination of 11 priority pollutant phenols in wastewater using dispersive liquid—liquid microextraction followed by high-performance liquid chromatography—diode-array detection. Analytical and Bioanalytical Chemistry. 2010 Feb 13;396(7):2685–93. doi: 10.1007/s00216-010-3496-z. 参考文献:10.1021/jo1000803 摘要:Benniston AC, Copley G, Harriman A, Howgego D, Harrington RW, Clegg W. Cofacial boron dipyrromethene (Bodipy) dimers: synthesis, charge delocalization, and exciton coupling. J Org Chem. 2010 Mar 19;75(6):2018–27. doi: 10.1021/jo1000803. 参考文献:10.1007/s10646-011-0731-0 摘要:Bhavsar SP, Awad E, Mahon CG, Petro S. Great Lakes fish consumption advisories: is mercury a concern Ecotoxicology. 2011 Oct;20(7):1588–98. doi: 10.1007/s10646-011-0731-0. 参考文献:10.1007/s11671-008-9174-9 摘要:Wu W, He Q, Jiang C. Magnetic Iron Oxide Nanoparticles: Synthesis and Surface Functionalization Strategies. Nanoscale Research Letters. 2008 Oct 02;3(11):397. doi: 10.1007/s11671-008-9174-9. 参考文献:10.1107/s160053681100715x 摘要:Duong MM, Tanski JM. 4-Bromo-N-(4-bromo-phen-yl)aniline. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o755.