2,5-二溴噻唑置于palladium On Activated Charcoal 氢气,Sodium Acetate体系中,用 甲醇 用作溶剂,化学反应 12.0H,以92%的收率获得噻唑 参考文献:Catalytic Hydrogenation Of Halothiazoles 标题:Catalytic Hydrogenation Of Halothiazoles 摘要:The Hydrogenation Of Halothiazoles Is Described. The Best Results Were Obtained Utilizing 10% Palladium On Carbon As Catalyst At Four Atmospheres Of Pressure With The Bromide Derivatives. Doi:10.1080/00397919508011485
专利信息
专利号:US-2008086013-A1 优先权日:2006-06-15 标 题:Carbometallation of alkynes and improved synthesis of uniquinones 发明人:LIPSHUTZ BRUCE H 权利人:UNIV CALIFORNIA 摘要:Methods for the carbometallation of alkynes are presented. Those are useful for the synthesis of CoQ 10 and other ubiquinones as well as for the synthesis of ubiquinol analogs.
专利号:US-5847150-A 优先权日:1996-04-24 标题 :Solid phase and combinatorial synthesis of substituted 2-methylene-2, 3-dihydrothiazoles and of arrays of substituted 2-methylene-2, 3-dihydrothiazoles 发明人:DORWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS 摘要:A solid phase method for the synthesis of a plurality of differently substituted 2-methylenethiazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 2-methylenethiazoles are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide under acidic conditions yields differently substituted, support-bound 2-methylene-2,3-dihydrothiazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 2-methylenethiazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:US-6117992-A 优先权日:1996-08-26 标题 :Reagents and process for synthesis of oligonucleotides containing phosphorodithioate internucleoside linkages 发明人:IYER RADHAKRISHNAN P 权利人:HYBRIDON INC 摘要:The invention provides new methods for synthesizing oligonucleotides containing at least one, and preferably all phosphorodithioate internucleoside linkages with less than 5% phosphoromonothioate contamination. This level of purity in the synthesis of phosphorodithoates has previously been very difficult to achieve with all existing methods. The invention further provides phosphorothioamidite nucleoside synthons comprising a sulfur protecting group that is stable under normal oligonucleotide synthesis conditions.
专利号:US-9126995-B2 优先权日:2011-11-08 标题:Method for catalytic asymmetric synthesis of optically active isoxazoline compound and optically active isoxazoline compound 发明人:TOYAMA KEN-ICHI; MORIYAMA YUJI; MATOBA KAZUTAKA; YAOSAKA MANABU; IKEDA EITATSU 权利人:NISSAN CHEMICAL IND LTD 摘要:There is provided a method for catalytic asymmetric synthesis of optically active isoxazoline compound and an optically active isoxazoline compound. A method for catalytic asymmetric synthesis of optically active isoxazoline compound of a formula (6) including reacting an α,β-unsaturated carbonyl compound of a formula (1) and a hydroxylamine in a solvent in the presence of a base by adding a chiral phase transfer catalyst. An optically active isoxazoline compound of a formula (13) that can be synthesized by the method.
专利号:US-8138346-B2 优先权日:2006-08-16 标题 :Method for synthesis of 8-alkoxy-9H-isothiazolo[5,4-B]quinoline-3,4-diones 发明人:BRADBURY BARTON JAMES; WILES JASON ALLAN; HASHIMOTO AKIHIRO; WANG QIUPING; LUCIEN EDLAINE; PAIS GODWIN; KIM HA YOUNG 权利人:BRADBURY BARTON JAMES; WILES JASON ALLAN; HASHIMOTO AKIHIRO; WANG QIUPING; LUCIEN EDLAINE; PAIS GODWIN; KIM HA YOUNG; ACHILLION PHARMACEUTICALS INC 摘要:The present invention provides process for synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones of the Formula A. n nThe substituents R, R 5 , R 6 , R 7 , R 8 and R 9 are defined herein. The invention also provides novel synthetic intermediates useful in the synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones.
专利号:US-5569762-A 优先权日:1994-01-14 标题:Asymmetric synthesis of intermediates for retroviral protease inhibitor compounds 发明人:WISSNER ALLAN; TROVA MICHAEL P 权利人:AMERICAN CYANAMID CO 摘要:The disclosure describes an improved process for producing optically active compounds of Formula II or III, which compounds are useful as intermediates for preparing compounds active as inhibitors of retroviral protease enzymes: ##STR1## wherein R 1 , R 50 and Z are described in the specification. The improved process includes either synthesis of diastereomeric iodolactones which are separated prior to conversion to compounds of Formula II or III or synthesis of an epoxide which is converted directly to compounds of Formula II and III.
参考文献:10.1128/aem.01790-09 摘要:Wang J, Yu Y, Tang K, Liu W, He X, Huang X, Deng Z. Identification and analysis of the biosynthetic gene cluster encoding the thiopeptide antibiotic cyclothiazomycin in Streptomyces hygroscopicus 10-22. Appl Environ Microbiol. 2010 Apr;76(7):2335–44. 参考文献:10.1016/j.bmc.2010.01.056 摘要:Mashkani B, Griffith R, Ashman LK. Colony stimulating factor-1 receptor as a target for small molecule inhibitors. Bioorg Med Chem. 2010 Mar 01;18(5):1789–97. doi: 10.1016/j.bmc.2010.01.056. 摘要:Liu B, Faia L, Hu M, Nussenblatt RB. Pro-angiogenic effect of IFNgamma is dependent on the PI3K/mTOR/translational pathway in human retinal pigmented epithelial cells. Mol Vis. 2010 Feb 10;16():184–93. 参考文献:10.1007/s00425-005-0171-2 摘要:Eom H, Lee CG, Jin E. Gene expression profile analysis in astaxanthin-induced Haematococcus pluvialis using a cDNA microarray. Planta. 2006 May;223(6):1231–42. doi: 10.1007/s00425-005-0171-2. 参考文献:10.1016/j.ijpharm.2011.06.046 摘要:Plajnšek KT, Pajk S, Govedarica B, Pečar S, Srčič S, Kristl J. A novel fluorescent probe for more effective monitoring of nanosized drug delivery systems within the cells. International Journal of Pharmaceutics. 2011 Sep;416(1):384–93. doi: 10.1016/j.ijpharm.2011.06.046.