Methyl 3-Oxo-3-(4-(Trifluoromethyl)Phenyl) Propanedithioate置于sodium Hydroxide体系中,用 水 作为反应溶剂,化学反应 9.0H,以97%的收率获得产物4-三氟甲基苯甲酸 参考文献:在无金属和无催化剂的条件下,通过c C键断裂和c O / C N / C S键形成,使二硫酯能够化学发散合成酸,酰胺和异噻唑 标题:在无金属和无催化剂的条件下,通过c C键断裂和c O / C N / C S键形成,使二硫酯能够化学发散合成酸,酰胺和异噻唑 摘要:首次设计了一种使用β-酮二硫酯的操作简单且用户友好的方法,可访问特权支架,例如酸,酰胺和异噻唑.值得注意的是,新方案涉及一锅中c C键断裂和c O / C N / N S键形成的组合.氨水导致骨骼上截然不同的酰胺和异噻唑的形成,而naoh水溶液则使芳香酸的形成接近定量产率.这种实用的方法可以极大地简化简单分子的合成,具有高度的化学选择性,成本效益,可克量级,对水分不敏感以及具有很高的官能团相容性. DOI:10.1016/j.Tetlet.2017.05.064
专利号:US-2015239796-A1 优先权日:2014-02-19 标题:One pot synthesis of 18f labeledtrifluoromethylated compounds with difluoro(iodo)methane 发明人:RüHL THOMAS; RISS PATRICK; RAFIQUE WAQAS 权利人:UNIV OSLO 摘要:The present invention relates to compositions and methods for the synthesis of 18 F labeled compounds. In particular, the present invention relates to a copper (I) mediated one pot method for 18 F-trifluoromethylation of aromatic- or heteroaromatic halides with difluoro(iodo)methane (e.g., for use at PET imaging agents).
专利号:US-7109377-B2 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products 发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R 权利人:HARVARD COLLEGE 摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
专利号:US-6245937-B1 优先权日:1996-11-29 标题 :Liquid phase parallel synthesis of chemical libraries 发明人:CHENG SOAN; SAUNDERS JOHN 权利人:DUPONT PHARMACEUTICALS RES LAB 摘要:This invention features methods of biphasic synthesis for synthesizing combinatorial libraries and combinatorial libraries of chemical compounds utilizing the template, and combinatorial libraries of chemical compounds formed by the methods of this invention.
专利号:US-6180830-B1 优先权日:1995-11-08 标题 :Method for preparing a bimetallic ruthenium/tin catalyst and a process for the synthesis of aldehydes 发明人:JACQUOT ROLAND 权利人:RHODIA CHIMIE SA 摘要:The present invention relates to a new process for the preparation of a bimetallic ruthenium/tin catalyst. The process for the preparation of a bimetallic ruthenium/tin catalyst according to the invention is characterised by the fact that it consists in carrying out the reduction of a ruthenium complex having an electrovalency of -4 and a coordination number of 6, the ligands being either a halogen atom or an anion or a tin halide. The catalyst is further employed for the preparation of aldehydes by reduction, in the vapor phase, of carboxylic acids, esters and anhydrides.
专利号:US-8114993-B2 优先权日:2007-02-06 标题:Use of aryl chlorides in palladium-catalyzed C-H bond functionalization 发明人:DAUGULIS OLAFS; CHIONG HENDRICH 权利人:DAUGULIS OLAFS; CHIONG HENDRICH; UNIV HOUSTON SYSTEM 摘要:A one-step method for efficiently converting carbon-hydrogen bonds into carbon-carbon bonds using chloroarenes and palladium catalysts is disclosed. This method allows faster introduction of complex molecular entities, a process that would otherwise require many more steps. This invention is particularly relevant for the organic synthesis of complex molecules such as, but not limited to, pharmacophores.
专利号:US-8242310-B2 优先权日:2008-09-10 标题:Processes for the preparation of aminosulfone compounds 发明人:SAINDANE MANOHAR T; GE CHUANSHENG 权利人:SAINDANE MANOHAR T; GE CHUANSHENG; CELGENE CORP 摘要:Processes for synthesizing aminosulfone compounds are provided. Aminosulfone compounds obtained using methods provided herein are useful in production or synthesis of isoindoline based PDE 4 modulators.
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合成参考文献
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