专利号:US-8853410-B2 优先权日:2009-04-30 标 题:Process for preparing substituted isoxazoline compounds and their precursors 发明人:RACK MICHAEL; KOERBER KARSTEN; KAISER FLORIAN 权利人:RACK MICHAEL; KOERBER KARSTEN; KAISER FLORIAN; BASF SE 摘要:The present invention relates to a new method of preparing halogenated styrene compounds of formula (VIII) n nwhich are precursors in the process of synthesis of substituted isoxazoline compounds of formula (I)n n nwherein R 1 to R 5 , R 8 and R 9 are described as in the description.n n The present invention relates further to the synthesis of compounds of formula (I) starting from acetophenones. The desired styrenes of formula are prepared from the appropriate substituted acetophenone. Asides bromo anilines react with formoxime. Obtained oximes undergo a cycloaddition with the styrenes and give isoxazolines. Compounds of formula (I) can then be prepared in a palladium catalyzed carbonylative amination reaction of the isoxazolines.
专利号:US-6531470-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:US-6562844-B2 优先权日:1998-01-23 标 题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:US-6417195-B1 优先权日:1999-02-22 标题 :Isoquinoline derivatives and isoquinoline combinatorial libraries 发明人:LEBL MICHAL 权利人:LION BIOSCIENCE AG 摘要:The present invention provides the synthesis of heterocyclic compounds based on the isoquinoline ring. More specifically, the invention provides novel isoquinoline derivatives as well as novel libraries comprised of such compounds.
专利号:US-5874443-A 优先权日:1995-10-19 标 题:Isoquinoline derivatives and isoquinoline combinatorial libraries 发明人:KIELY JOHN S; GRIFFITH MICHAEL C 权利人:TREGA BIOSCIENCES INC 摘要:The present invention provides the synthesis of heterocyclic compounds based on the isoquinoline ring. More specifically, the invention provides novel isoquinolines as well as novel libraries comprised of many such compounds, and methods of synthesizing the libraries.
专利号:US-7002020-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
摘要:Gosmini, C.; Corpet, M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 631. 摘要:Mori, Y.; Kobayashi, S., Science of Synthesis: Water in Organic Synthesis, (2012) 1, 835. 摘要:A. de Courville. Compt. Rend., C 262, 1196 (1966).