2,4-二氯-6-甲基嘧啶置于碘,锌体系中,用 乙醇,水 用作溶剂,化学反应 4.0H,以53%的收率获得2-氯-4-甲基嘧啶 参考文献: Thiazole And Oxazole Kinase Inhibitors[fr] Inhibiteurs De Kinase à Base De Thiazole Et D'Oxazole 标题: Thiazole And Oxazole Kinase Inhibitors[fr] Inhibiteurs De Kinase à Base De Thiazole Et D'Oxazole 摘要:本发明提供了噻唑和恶唑化合物,含有该化合物的组合物,以及它们的制备方法和作为药物的应用方法.
专利信息
专利号:US-8242273-B2 优先权日:2005-07-28 标 题:Synthesis of 4/5-pyrimidinylimidazoles via sequential functionalization of 2,4-dichloropyrimidine 发明人:DENG XIAOHU; MANI NEELAKANDHA 权利人:DENG XIAOHU; MANI NEELAKANDHA; JANSSEN PHARMACEUTICA NV 摘要:This invention relates to methods of making pyrimidinyl-substituted imidazole compounds by sequential substitution of the 4- and 2-chloro groups of 2,4-dichloropyrimidine, nucleophilic substitution to form pyrimidinylalkyne derivatives, oxidation to the corresponding 1,2-diketones, and cyclocondensation reactions.
专利号:US-9533959-B2 优先权日:2013-10-07 标 题:Methods of regioselective synthesis of 2,4-disubstituted pyrimidines 发明人:CHARRIER JEAN-DAMIEN; O'DONNELL MICHAEL EDWARD 权利人:VERTEX PHARMA 摘要:The present invention relates to the novel regioselective syntheses of 2,4-disubstituted pyrimidines through sequential nucleophilic aromatic substitutions.
专利号:US-8853410-B2 优先权日:2009-04-30 标 题:Process for preparing substituted isoxazoline compounds and their precursors 发明人:RACK MICHAEL; KOERBER KARSTEN; KAISER FLORIAN 权利人:RACK MICHAEL; KOERBER KARSTEN; KAISER FLORIAN; BASF SE 摘要:The present invention relates to a new method of preparing halogenated styrene compounds of formula (VIII) n nwhich are precursors in the process of synthesis of substituted isoxazoline compounds of formula (I)n n nwherein R 1 to R 5 , R 8 and R 9 are described as in the description.n n The present invention relates further to the synthesis of compounds of formula (I) starting from acetophenones. The desired styrenes of formula are prepared from the appropriate substituted acetophenone. Asides bromo anilines react with formoxime. Obtained oximes undergo a cycloaddition with the styrenes and give isoxazolines. Compounds of formula (I) can then be prepared in a palladium catalyzed carbonylative amination reaction of the isoxazolines.
专利号:US-2010274015-A1 优先权日:2005-07-28 标 题:Synthesis of 4/5-pyrimidinylimidazoles via sequential functionalization of 2,4-dichloropyrimidine
专利号:US-2007027319-A1 优先权日:2005-07-28 标 题 :Synthesis of 4/5-pyrimidinylimidazoles via sequential functionalization of 2,4-dichloropyrimidine
专利号:US-10005737-B2 优先权日:2013-10-07 标题:Methods of regioselective synthesis of 2,4-disubstituted pyrimidines