专利号:WO-2005121077-A1 优先权日:2004-06-10 标题:Preparation and applications of polymer-supported halogenated benzoquinones as oxidative agents 发明人:COULADOUROS ELIAS; STRONGILOS ALEXANDROS 权利人:COULADOUROS ELIAS; STRONGILOS ALEXANDROS 摘要:This invention provides a general method for the synthesis of polymer-supported benzoquinones described by the following generic structure I: wherein: •, X, R1, R2 and R3 are described in the main text. The general concept of the method consists of the use of a halogenated starting material of the general structure II (Figure 1) which by an nucleophilic substitution reaction (NSR) or a palladium mediated coupling (PMC) is either directly loaded on a resin to afford IIIa (Path A) or transformed to intermediate IIIb (Path B) which is subsequently (with or without modification) loaded on a resin to afford once again IIIa. Deprotection and/or oxidation of IIIa, if needed, afford target solid-supported oxidants I The polymer-supported benzoquinones I are used for the oxidation of hydroquinones to quinones, for the oxidation of benzylic alcohols the aldehydes, for the removal of p-methoxybenzyl and related protective groups, for the dehydrogenation of tetrahydronaphthalene derivatives and for the dehydrogenation of steroid 4-en-3-ones. The polymer-supported reagent after its use is regenerated upon treatment with an oxidative agent.
专利号:US-8461298-B2 优先权日:2004-11-01 标 题:Compositions and methods for modification of biomolecules 发明人:BERTOZZI CAROLYN R; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL 权利人:BERTOZZI CAROLYN R; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL; UNIV CALIFORNIA 摘要:The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).
专利号:US-4226800-A 优先权日:1979-06-14 标 题 :Synthesis of acetylene-terminated compounds 发明人:PICKLESIMER LEWELLYN G 权利人:US AIR FORCE 摘要:Phenolic materials containing propargyl groups are prepared by reacting a polyhydric, phenolic material with propargyl bromide, the reaction being conducted in an aqueous sodium hydroxide solution. The products can be thermally polymerized to polymers which are useful as adhesives and as matrix resins in the fabrication of composites.
专利号:US-12071422-B2 优先权日:2022-02-07 标 题 :Process for synthesis of quinazoline compounds 发明人:LEBL RENE; LIM NGIAP KIE; MEIER ROLAND CHRISTOPH; ORCEL UGO JONATHAN; SEDELMEIER JOERG; SHEN JEFF; SIROIS LAUREN ELIZABETH; TIMMERMAN JACOB C; TRACHSEL ETIENNE; WHITE NICHOLAS ANDREW; XU JIE; ZHANG HAIMING; BACHMANN STEPHAN; BASS THOMAS MICHAEL; BIGLER RAPHAEL; BURKHARD JOHANNES ADRIAN; CLAGG KYLE BRADLEY PASCUAL; GOSSELIN FRANCIS; HAN CHONG; KALDRE DAINIS; KELLY SEAN M; HEROLD SEBASTIAN; LEITNER CHRISTIAN 权利人:GENENTECH INC; HOFFMANN LA ROCHE 摘要:Provided herein are methods to synthesize compounds useful in the treatment of cancer where such compounds comprise a quinazolinyl core moiety and at least one stereoisomeric or atropisomeric moiety.
专利号:US-9260371-B2 优先权日:2004-11-01 标题:Compositions and methods for modification of biomolecules 发明人:BERTOZZI CAROLYN RUTH; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL; SLETTEN ELLEN MAY 权利人:UNIV CALIFORNIA 摘要:The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).
专利号:CN-105646641-A 优先权日:2016-02-26 标题:Formation method of 1,2 double bond in the synthesis of finasteride and dutasteride