(R,S) Tert-Butyl 2-{1-[3,4-Difluoro-2-(2-Fluoro-4-Iodophenylamino)Benzoyl]-3-Hydroxy-3-Azetidinyl}-1-Piperidinecarboxylate 以99的收率获得产物2,3,4-三氟苯甲酸 参考文献:Modulators Of Pharmacokinetic Properties Of Therapeutics 标题:Modulators Of Pharmacokinetic Properties Of Therapeutics 摘要:本申请提供了公式i的化合物,或其药学上可接受的盐,溶剂合物和/或酯,含有这种化合物的组合物,包括这种化合物的治疗方法,以及包括这种化合物与至少一种额外治疗剂的治疗方法.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:WO-9731891-A1 优先权日:1996-03-01 标 题:Process for regioselective substitution of trifluorobenzoate or trifluorobenzonitrile 发明人:LYNCH JOSEPH E; SHI YAO-JUN; WELLS KENNETH M 权利人:MERCK & CO INC; LYNCH JOSEPH E; SHI YAO JUN; WELLS KENNETH M 摘要:The invention provides a process for regioselective substitution of trifluorobenzoate/trifluorobenzonitrile to afford the difluorobenzoate/difluorobenzonitrile in good yields. The resulting difluorobenzoate/difluorobenzonitrile can again be regioselectively substituted with a second nucleophile to give monofluorobenzoate/monofluorobenzonitrile also in good yields. This process is particularly useful for forming key intermediates in the synthesis of oxytocin antagonist compounds.
专利号:WO-2024126692-A1 优先权日:2022-12-15 标题 :Peracid promoters in the iridium-catalyzed hydrosilylation synthesis of haloalkylorganosilanes 发明人:SCHOLZ HENRIK; KROKE EDWIN; KRAUSHAAR KONSTANTIN; GLATZER HOLGER JÜRGEN; LEWIS KENRICK MARTIN; WAGNER ROLAND 权利人:MOMENTIVE PERFORMANCE MAT GMBH 摘要:The present invention is directed at a process for producing a compound of Formula (I): (R1)y(R2O)3-ySiCH2CHR3CR4R5X comprising reacting (a) an olefinic halide; (b) an alkoxysilane; (c) a catalytically effective amount of iridium-containing catalyst; and (d) a reaction-promoting effective amount of a peroxycarboxylic acid to produce the product of Formula (I).
专利号:US-5777123-A 优先权日:1996-03-01 标题 :Process for regioselective substitution of trifluorobenzoate or trifluorobenzonitrile 发明人:LYNCH JOSEPH E; SHI YAO-JUN; WELLS KENNETH M 权利人:MERCK & CO INC 摘要:The invention provides a process for regioselective substitution of trifluorobenzoate/trifluorobenzonitrile to afford the difluorobenzoate/difluorobenzonitrile in good yields. The resulting difluorobenzoate/difluorobenzonitrile can again be regioselectively substituted with a second nucleophile to give monofluorobenzoate/monofluorobenzonitrile also in good yields. This process is particularly useful for forming key intermediates in the synthesis of oxytocin antagonist compounds.
专利号:US-2024091733-A1 优先权日:2022-09-02 标题 :System of modular kits to produce chemical targets of interest 发明人:CHOI EUGENE; RAPP KERSTEN; HAMMERSMITH GREG; CREGGER BRIAN 权利人:ODH IP CORP 摘要:This disclosure provides systems and methods for the on-demand synthesis, separation, purification and formulation of chemicals, and particularly for the on-demand production of pharmaceutical products. More particularly, the disclosure provides continuous-flow on-demand systems, comprising one or more reagent holding/dispensing containers, continuous-flow chemical synthesis modules and/or one or more separation, crystallization, filtration, wash and/or formulation modules, additionally comprising automated detection systems and methods for monitoring reagents, products and processing parameters and automated control systems and methods for controlling processing conditions and parameters.
专利号:US-2014170151-A1 优先权日:2010-04-23 标 题:Synthetic Oligosaccharides for Staphylococcus Vaccine 发明人:CAMPBELL A STEWART; PLANTE OBADIAH J 权利人:CAMPBELL A STEWART; PLANTE OBADIAH J 摘要:The present invention synthetic oligo-β-(1→6)-glucosamine structures and a methodology which essentially allows for the synthesis of any oligo-β-(1→6)-glucosamine species having a definite number of monosaccharide units, including a set pattern of acetylated and non-acetylated residues. The invention further provides antibodies to these synthetic oligo-β-(1→6)-glucosamines as well as compositions thereof and methods for treating and preventing infections caused by bacteria expressing poly-β-(1→6)-glucosamines, such as Staphylococcus aureus.