专利号:US-2013172553-A1 优先权日:2009-11-25 标题 :Chiral synthesis of isoxazolines, isoxazoline compounds, and uses thereof 发明人:SIELECKI-DZURDZ THAIS; PRUITT JAMES 权利人:SIELECKI-DZURDZ THAIS; PRUITT JAMES; CPSI STOCKHOLDER TRUST 摘要:Processes for the chiral syntheses of isoxazolines and intermediates are described. Compounds prepared thereby, and methods of using the compounds are also described.
专利号:US-2018148745-A1 优先权日:2015-05-26 标题:Hemoprotein catalysts for improved enantioselective enzymatic synthesis of ticagrelor 发明人:ARNOLD FRANCIS H; RENATA HANS; MCINTOSH JOHN A; LEWIS RUSSELL D; KAN SEK BIK JENNIFER; HERNANDEZ KARI; COELHO PEDRO; ROZZELL DAVID; ZHANG CHEN 权利人:CALIFORNIA INST OF TECHN; PROVIVI INC 摘要:The present invention provides methods by which trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine and related cyclopropane compounds are prepared using synthetic strategies that include a biocatalytic cyclopropanation step.
专利号:US-8487108-B2 优先权日:2005-11-14 标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors 发明人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T 权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC 摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
专利号:WO-2015067230-A1 优先权日:2013-11-08 标题 :A production method and a new crystalline form of an intermediate of synthesis of ticagrelor 发明人:VOSLAR MICHAL; STRELEC IVO; DAMMER ONDREJ; VYSLOUZIL ROSTISLAV; STEHLĺČEK, Ivan; RIHA JAROSLAV; HES TOMAS; OBADALOVA IVA 权利人:ZENTIVA KS 摘要:The invention relates to preparation of ticagrelor of formula I and comprises a reaction of a compound of formula IV with a deprotection agent in a solvent to a compound of formula V, which is advantageously isolated by crystallization and subsequently used for the preparation of ticagrelor. The substituent R in formulae IV and V is CH 2 CH 2 OH, CH 2 COOH, or CH 2 COOR 1 ; R 1 is a branched or unbranched R1-C4 alkyl; and X is NH 2 , NO 2 f or NHCHO.
专利号:WO-2018109082-A1 优先权日:2016-12-15 标题 :Process and intermediate for the preparation of 1-(4-(2-((1-(3,4- difluorophenyl)-1h-pyrazol-3-yl)methoxy)ethyl)piperazin-1-yl)ethanone 发明人:ALMANSA ROSALES CARMEN; CAAMAÑO MOURE ANA MARÃ?A; ENJO BABÃ?O JUAN 权利人:ESTEVE LABOR DR 摘要:The present invention relates to a process for the preparation of 1-(4-(2-((1-(3,4-difluorophenyl)-1H-pyrazol-3-yl)methoxy)ethyl)piperazin-1-yl)ethanone and salts and solvates thereof and to the use of intermediates in the synthesis of these compounds. Also is provided a new intermediate compound.
专利号:US-7060818-B2 优先权日:2003-02-21 标题:Synthesis of macrocyclic tetraamido compounds and new metal insertion process 发明人:HORWITZ COLIN P; GHOSH ANINDYA 权利人:UNIV CARNEGIE MELLON 摘要:An improved method of synthesizing a macrocyclic tetraamido compound includes protecting the amino portion of an amino carboxylic acid to form a protected amino carboxylic acid; exposing the protected amino carboxylic acid to a first solvent, preferably a hydrocarbon solvent, such as toluene or 1,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane. The carboxylic acid portion of the protected amino carboxylic acid is then converted to an activated carboxylic acid by one of esterification or acid halide formation, to form a protected amino activated carboxylic acid derivative. The protected amino activated carboxylic acid derivative is reacted with a diamine in the presence of a second solvent, such as THF or ,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane, to form a protected diamide diamine intermediate. Following deprotection, the diamide diamine intermediate is reacted with an activated diacid, such as an activated malonate, oxalate or succinate derivative to form the macrocyclic tetraamido compound. The macrocyclic tetraamido compound may further be complexed with a transition metal.
参考文献:10.1055/s-2008-1032088 摘要:Naidu B. Tandem Retro-Michael Addition-Claisen Rearrangement-Intramolecular Cyclization: One-Pot Synthesis of Densely Functionalized Ethyl Dihydropyrimidine-4-carboxylates from Simple Building Blocks. Synlett. 2008 Feb 12;2008(04):547–50. doi: 10.1055/s-2008-1032088. 参考文献:10.1055/s-0032-1316578 摘要:Zhang J, Zhu S, Shang W, Chen X, Zou Y, He S, Zhao J. Preparation of Pentafluorinated Phenyl-Monohydro[60]fullerenes. Synthesis. 2012 Jul 06;44(16):2575–8. doi: 10.1055/s-0032-1316578.