对溴氟苯置于magnesium体系中,用 四氢呋喃 作为反应溶剂,化学反应生成 4-氟苯基溴化镁 参考文献:C(sp3)-c(sp3)σ键的简便氢解 标题:C(sp3)-c(sp3)σ键的简便氢解 摘要:通过钯催化的c(sp 3)-c(sp 3)氢解对苄基的季碳,叔碳和仲碳中心进行修饰)呈现σ键.当在温和的氢解条件下(含钯碳和氢气的大气压)处理带有季苄基中心的苄基麦德鲁姆的酸衍生物时,就可以很好地获得高收率的芳族化合物,这些芳族化合物被叔苄基中心和麦德鲁姆酸所取代.类似地,含有叔或仲苄基中心的底物分别产生被仲苄基中心或甲苯衍生物取代的芳族化合物.此外,该策略用于二芳基甲烷的高产率合成.探索了还原性脱烷基反应的范围,并确定了对空间和电子因素的限制.描述了该反应的机理分析,该分析由氘标记实验和对映体富集的衍生物的氢解组成.调查显示,C(sp 3)-c(sp 3)σ键断裂事件是通过混合的s N 1 / S N 2机理发生的,其中钯中心置换了一个基于碳的离去基团,即meldrum酸,其构型反转,随后通过还原消除钯来提供ch键. DOI:10.1002/adsc.201600535
专利信息
专利号:US-2008119662-A1 优先权日:2004-02-16 标 题:One Spot Synthesis of Citalopram from 5-Cyanophthalide 发明人:NARAHARI BABU AMBATI; SRINIVAS GOUD VUDDAMARI; GAONKAR SANTOSH LAXMAN; MANJUNATHA SULUR G; KULKARNI ASHOK KRISHNA; KULKARNI MADHARI A 权利人:JUBILANT ORGANOSYS LIMTED 摘要:A process for one pot synthesis of citalopram is disclosed. The process comprises subjecting 5-cyano phthalide to Grignard reduction followed cyclization and followed by C-alkylation reaction to obtain citalopram without isolation and purification of any intermediates. In another embodiment, 5-cyano phthalide is subjected to sequential Grignard reactions followed by cyclization to obtain citalopram without isolation and purification of any intermediate stages.
专利号:EP-2918579-A1 优先权日:2014-03-14 标题 :Synthesis of 2-arylmethyl-5-aryl-thiophene 权利人:LEK PHARMACEUTICALS 摘要:The present invention provides a new synthetic process for the production of 2-arylmethyl-5-aryl-thiophene, an intermediate in the synthesis of C-aryl glycosides.
专利号:WO-9964428-A1 优先权日:1998-06-10 标题:Synthesis of aryl boronic acids 发明人:SULLIVAN JEFFREY M; BARNES HAMLIN H 权利人:BOULDER SCIENT CO; SULLIVAN JEFFREY M; BARNES HAMLIN H 摘要:A method for synthesis of aryl boronic acids is disclosed.
专利号:US-6600040-B2 优先权日:2000-06-08 标 题:Process for the synthesis of (2R, 2-alpha-R, 3A)-2-[1-(3,5-bis(trifluoromethyl)phenyl)ethoxy]-3-(4-fluorophenyl)-1, 4-oxazine 发明人:BRANDS KAREL M JOS; TSAY FUH-RONG; CONRAD KAREN M; ZHAO MATTHEW M 权利人:MERCK & CO INC 摘要:The present invention is concerned with novel processes for the preparation of (2R, 2-alpha-R, 3a)-2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy-3-(4-fluorophenyl)-1,4-oxazine. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
专利号:US-8835476-B2 优先权日:2005-03-04 标 题:Synthesis of novel antimicrobials 发明人:WU FAN; WEAVER DONALD; BARDEN CHRIS; MCMASTER CHRISTOPHER; BYERS DAVID; HENNEBERRY ANNETTE; BAN FUQIANG 权利人:WU FAN; WEAVER DONALD; BARDEN CHRIS; MCMASTER CHRISTOPHER; BYERS DAVID; HENNEBERRY ANNETTE; BAN FUQIANG 摘要:The synthesis and activity of novel LpxA inhibitors is described, these inhibitors present antibacterial activity. The compounds were designed based on a receptor model developed using the crystal structure of LpxA and are arranged to have a favorable binding interaction at the active site of the enzyme. In particular, the compounds present the following formula (I) where V, W, X, Y and Z can be independently C, S, N or O and P1, P2 and P3 are ligands to bind to the three points of the proposed pharmacophore model. They can be chosen from a variety of groups.
专利号:WO-2014011120-A1 优先权日:2012-07-13 标 题 :Endoperoxides, synthesis and uses thereof for the treatment of neoplastic diseases such as cancer 发明人:TAN NGUAN SOON; CHIBA SHUNSUKE 权利人:UNIV NANYANG TECH 摘要:The present invention generally relates to processes and methods for the synthesis of endoperoxide compounds. More specifically, the invention relates to a method for preparing endoperoxide compounds starting from an aryl imine of formula (I) in the presence of a metallic catalyst and oxygen. The present invention also relates to endoperoxide compounds of formula (III) and their pharmaceutically acceptable salts thereof, useful for therapy. All substituents are defined herein. Also disclosed are methods of treating cancer using the compounds of formula (III).
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