CAS: 220880-12-6; 4-(Trifluoromethyl)Pyrimidine-5-Carboxylic Acid

相似化合物

1260676-79-6 1803738-77-3 187035-81-0

上下游产品

CAS号425392-76-3 5-溴-4-氯-6-(三氟甲基)嘧啶 | CAS号1546-78-7 4-羟基-6-(三氟甲基)嘧啶 | CAS号37552-81-1 4-氯-6-三氟甲基嘧啶 | CAS号785777-94-8 4,5-二溴-6-三氟甲基嘧啶 | CAS号126538-81-6 5-溴-6-三氟甲基嘧啶-4-酮

4-Chloro-6-(Trifluoromethyl)Pyrimidine-5-Carboxylic Acid置于palladium On Activated Charcoal 氢气,三乙胺体系中,用 甲醇 用作溶剂,25.0 °C,101.32 Kpa 条件下,反应 2.0H,以83%的收率获得4-(三氟甲基)嘧啶-5-羧酸
参考文献:含金属和三氟甲基取代的嘧啶:生成和功能化
标题:含金属和三氟甲基取代的嘧啶:生成和功能化
摘要:当金属两侧有两个吸电子取代基(如三氟甲基和氯或溴)时,5-嘧啶基锂物种相当稳定.因此,在用异丙基氯化镁完成卤素/金属置换后,由 4,5-二溴-6-(三氟甲基)嘧啶和 5-溴-4-氯-6-(三氟甲基)嘧啶以高产率生产相应的 5-羧酸或丁基锂,然后羧化.当 4-氯-,2,4-二氯-和 2,4-二溴-6-(三氟甲基)嘧啶在与干冰反应之前用二异丙基氨基锂去质子化时,同样获得令人满意或优异的 5-羧酸产率. 相比之下,用丁基锂连续处理 2-Bromo-4-(Trifluoromethyl)Pyrimidine 和 2-Chloro-5-Iodo-4-(Trifluoromethyl)Pyrimidine 得到了预期的羧酸,收率很低,甚至没有痕量的 Amts.当 4-溴-6-(三氟甲基)嘧啶作为底物时,检测到酸.从两个相互竞争的机制途径中的任何一个中出现的双嘧啶的形成是一种永久性的有害副反应.[在 Scifinder
Doi:10.1002/ejoc.200500848

专利信息

专利号:US-6562844-B2
优先权日:1998-01-23
标 题:Oxazolidinone combinatorial libraries, compositions and methods of preparation
发明人：GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC
权利人:UPJOHN CO
摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.