对苯二甲醚置于n-溴代丁二酰亚胺(Nbs)体系中,用 乙腈 用作溶剂,以96%的收率获得1-溴-2,5-二甲氧基苯 参考文献:Synthesis Of Arylbromides From Arenes And N-Bromosuccinimide (Nbs) In Acetonitrile-A Convenient Method For Aromatic Bromination 标题:Synthesis Of Arylbromides From Arenes And N-Bromosuccinimide (Nbs) In Acetonitrile-A Convenient Method For Aromatic Bromination 摘要:利用乙腈中的 N-溴代丁二酰亚胺(nbs),可以很容易地对一系列活化的炔类化合物进行区域选择性和化学选择性亲电溴化反应.与其他亲电溴化条件相比,该方法的环境友好,底物范围大且易于合成,从而提高了其实用性. Doi:10.1139/v08-176
专利号:US-6355826-B1 优先权日:1997-09-17 标题:Synthesis of stable nitrile oxide compounds 发明人:PARKER DANE KENTON 权利人:GOODYEAR TIRE & RUBBER 摘要:This invention discloses a process for the synthesis of stable aryl nitrile oxides which comprises the sequential steps of (1) halomethylating a halomethyl group onto a substituted aromatic compounds wherein said halomethyl group is halomethylated onto a position that is ortho to at least one of the substituent groups on the substituted aromatic compound; (2) converting the ortho halomethylated-substituted aromatic compound into an ortho-substituted aromatic aldehyde by reacting the ortho halomethylated-substituted aromatic compound with a salt selected from the group consisting of sodium 2-nitropropane and potassium 2-nitropropane in a lower alcohol solvent; (3) converting the ortho-substituted aromatic aldehyde into an ortho-substituted aromatic; and (4) converting the ortho-substituted aromatic oxime into the ortho-substituted aryl nitrile oxide by reacting the ortho-substituted aromatic oxime with an aqueous sodium hypochlorite solution.
专利号:US-7094928-B2 优先权日:2002-08-21 标题 :Process for the synthesis of (±) 2-Amino-N-[2,(2,5-dimethoxy phenyl)-2-hydroxyethyl] acetamide monohydrochloride 发明人:SUBRAMANIAN RAJARAM SANKARA; SATAGOPAN VENKATANATHAN; SRINIVASAN RAJAGOPALAN 权利人:SANMAR SPECIALTY CHEMICALS LTD 摘要:This invention relates to an improved process for synthesizing (±)-2-Amino-N-[2-(2,5-dimethoxyphenyl]-2-hydroxyethyl acetamide monohydrochloride in good yield and in a cost effective manner from 1-(2,5-dimethoxyphenyl)-2-bromoethanone by reacting the same with hexamine in the presence of novel solvent system comprising Tetrahydrofuran and water. The resulting aminoethanone is acylated with haloacetylchloride and sodium acetate in acetone-water solvent system. This product is reduced selectively first with sodium borohydride and subsequently with stannous chloride. This product is converted in situ to the corresponding hydrochloride salt immediately after reduction on its own.
专利号:US-9428500-B2 优先权日:2012-05-11 标 题 :Alpha-carbolines for the treatment of cancer 发明人:GAMBACORTI-PASSERINI CARLO; MOLOGNI LUCA; SCAPOZZA LEONARDO; BISSON WILLIAM; AHMED SHAHEEN; GOEKJIAN PETER; TARDY SÉBASTIEN; ORSATO ALEXANDRE; GUEYRARD DAVID; BENOIT JOSEPH 权利人:UNIVERSITA' DEGLI STUDI DI MILANO—BICOCCA; UNIV GENEVE; UNIVERSITÉ CLAUDE BERNARD—LYON 1; UNIV DEGLI STUDI DI MILANO—BICOCCA; UNIV GENEVE; UNIV CLAUDE BERNARD—LYON 摘要:The present invention relates to inhibitors of the oncogenic protein kinase ALK of formula (I) as herein described and pharmaceutical compositions thereof, as well as to key intermediates towards their synthesis. The compounds of formula (I) are useful in the preparation of a medicament, in particular for the treatment of cancer.
专利号:CA-2245780-A1 优先权日:1997-09-17 标 题 :Synthesis of stable nitrile oxide compounds
专利号:JP-2000508664-A 优先权日:1996-04-22 标题:Solid-phase and combinatorial synthesis of substituted thiophenes and arrays of substituted thiophenes
专利号:US-7615634-B2 优先权日:2003-02-10 标题:4-aminopyrimidine-5-one derivatives 发明人:BARTKOVITZ DAVID JOSEPH; CHU XIN-JIE; DING QINGJIE; JIANG NAN; LOVEY ALLEN JOHN; MOLITERNI JOHN ANTHONY; MULLIN JR JOHN GUILFOYLE; VU BINH THANH; WOVKULICH PETER MICHAEL 权利人:HOFFMANN LA ROCHE 摘要:Novel intermediate compounds are disclosed. These compounds are useful in the synthesis of 4-aminopyrimidine-5-one derivatives that inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). The 4-aminopyrimidine-5-one derivatives and their pharmaceutically acceptable salts have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors.
摘要:Yoshikai, N.; Rayner, C. M.; Graham, M. A., Science of Synthesis Knowledge Updates, (2020) 2, 55. 摘要:Virieux, D.; Ayad, T.; Pirat, J.-L.; Volle, J.-N., Science of Synthesis Knowledge Updates, (2018) 1, 256. 摘要:Carboni, B.; Carreaux, F., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 276. 摘要:Melkonyan, F. S.; Gevorgyan, V., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 1, 21. 摘要:Selt, M.; Waldvogel, S. R., Science of Synthesis: Special Topics, (2021) 1, 280.