专利号:US-7301006-B2 优先权日:2002-07-16 标 题 :Methods and materials for the synthesis of modified peptides 发明人:YOUNG TRAVIS G; KIESSLING LAURA L 权利人:WISCONSIN ALUMNI RES FOUND 摘要:Methods and protected amino acids useful as building blocks (protected monomers) for the synthesis of peptides and proteins that are selectively modified at one or more side-chain hydroxyl groups. Azide-bearing protecting groups allow the selective deprotection of side-chain hydroxyl groups of amino acids after synthesis of a peptide. Reaction conditions for removal of the azide-bearing protecting group can be selected which are substantially orthogonal to those that will remove α-amino protecting groups typically employed in peptide synthesis, such that hydroxyl groups protected with the azide-bearing protecting group remain protected during synthesis of the peptide chain. Various protecting groups which are readily available can be used for protecting potentially reactive side chain groups of amino acids in the peptide or protein to be modified. Preferred side-chain protecting groups are chemically distinguishable from the azide-bearing protecting group and substantially orthogonal reaction conditions can be selected such that side-chain protection of other amino acids is maintained when the azide-bearing protecting group is removed. The use of the azide-bearing protecting group of this invention for one or more hydroxy amino acids during peptide synthesis allows the selective unmasking of those azide-protected side-chain hydroxyl groups and selective modification of the hydroxyl groups that are selectively unmasked. The methods and materials herein are particularly used in synthesis of sulfated, phosphorylated and glycosylated peptides and proteins. Kits and methods of synthesizing a modified peptide or protein using the kits are also provided.
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-2012165520-A1 优先权日:2010-12-23 标题:Process for the synthesis of prodrugs of opioids 发明人:MCGEE PAUL; GARNETT IAN; JUAN E; MANAGE A; CARNIAUX JEAN-FRANCOIS 权利人:MCGEE PAUL; GARNETT IAN; JUAN E; MANAGE A; CARNIAUX JEAN-FRANCOIS 摘要:The present invention provides a process for the synthesis of opioid prodrugs. In particular, the present invention provides a process for the synthesis of opioid prodrugs comprising: treating an opioid, in the form of a salt or a freebase, with a carbonyl synthon to form an activated intermediate and subsequently reacting the activated intermediate with an amine, in the form of a salt or a freebase.
专利号:US-6117992-A 优先权日:1996-08-26 标题 :Reagents and process for synthesis of oligonucleotides containing phosphorodithioate internucleoside linkages 发明人:IYER RADHAKRISHNAN P 权利人:HYBRIDON INC 摘要:The invention provides new methods for synthesizing oligonucleotides containing at least one, and preferably all phosphorodithioate internucleoside linkages with less than 5% phosphoromonothioate contamination. This level of purity in the synthesis of phosphorodithoates has previously been very difficult to achieve with all existing methods. The invention further provides phosphorothioamidite nucleoside synthons comprising a sulfur protecting group that is stable under normal oligonucleotide synthesis conditions.
专利号:WO-0027627-A1 优先权日:1998-11-12 标题 :Aryloxime linkers in the solid-phase synthesis of 3-aminobenzisoxazoles 发明人:WILEY MICHAEL ROBERT; LEPORE SALVATORE DONATO 权利人:LILLY CO ELI; WILEY MICHAEL ROBERT; LEPORE SALVATORE DONATO 摘要:In its first aspect, the invention is directed to a solid support mediated method for the synthesis of diverse polycyclic heterocycles according to general formula (V). A second aspect of the invention is directed to a solid support bound intermediate compound that optionally can be derivatized before a cyclization and displacement procedure provides a product. The intermediate is preferably stable to a wide range of chemical conditions thus allowing, if desired, for the chemical derivatization of the intermediate. A third aspect of the invention is directed to a library of polycyclic heterocycle compounds where said library contains a plurality of diverse library compounds of general formula (V). A fourth aspect of the invention is directed to a method for the synthesis of a library of diverse polycyclic heterocycles by the general method described. A fifth aspect of the invention is directed to an assay kit for the identification of lead compounds of the library described therein.
专利号:US-10053406-B2 优先权日:2015-10-23 标题 :Synthesis of honokiol 发明人:JARACZ STANISLAV; KOZLOWSKI MARISA; EUN LEE YOUNG; KIM SUN MIN 权利人:COLGATE PALMOLIVE CO; UNIV PENNSYLVANIA 摘要:Disclosed herein are improved methods for the synthesis of honokiol, as well as methods for the synthesis of 3,3′-di-tert-butyl-5,5′-dimethyl-[1,1′-biphenyl]-2,4′-diol, 3′,5-dimethyl-[1,1′-biphenyl]-2,4′-diol, and 2,4′-dimethoxy-3′,5-dimethyl-1,1′-biphenyl, 3,3′,5,5′-tetra-tert-butyl-[1,1′-biphenyl]-2,4′-diol, and certain tetrasubstituted bisphenols, and uses therefor.
摘要:Kostikov, R. R.; Khlebnikov, A. F.; Sokolov, V. V., Science of Synthesis, (2010) 47, 788. 摘要:Sandford, G., Science of Synthesis Knowledge Updates, (2012) 2, 492. 参考文献:10.1007/s00253-002-1011-y 摘要:Janikowski TB, Velicogna D, Punt M, Daugulis AJ. Use of a two-phase partitioning bioreactor for degrading polycyclic aromatic hydrocarbons by a Sphingomonas sp. Appl Microbiol Biotechnol. 2002 Jul;59(2-3):368–76. doi: 10.1007/s00253-002-1011-y. 参考文献:10.1016/j.jchromb.2005.11.010 摘要:Chen YL, Hirabayashi H, Akhtar S, Pelzer M, Kobayashi M. Simultaneous determination of three isomeric metabolites of tacrolimus (FK506) in human whole blood and plasma using high performance liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2006 Jan 18;830(2):330–41. doi: 10.1016/j.jchromb.2005.11.010.