CAS: 170886-13-2; 2-(Trifluoromethyl)Pyridin-4-Ol

相似化合物

43150-55-6 1805320-30-2 1622843-95-1

上下游产品

2-(trifluoromethyl)-4H-pyran-4-one methyl 3-chloro-5-cyclopropyl-7-(trifluoromethyl)pyrazolo[1,5-a]pyridine-2-carboxylate 3-chloro-5-cyclopropyl-7-(trifluoromethyl)pyrazolo[1,5-a]pyridine-2-carboxylic acid 1-(3-methylcyctopentyl)-2-piperazinone hydr°Chloride 4-(4-nitrophenoxy)-2-(trifluoromethyl)pyridine 4-{2-[2,6-dichloro-4-(3,3-dichloroallyloxy)-benzyloxy]-ethoxy}-2-trifluoromethyl-pyridine 5-nitro-2-(trifluoromethyl)pyridin-4-ol 5-iodo-2-(trifluoromethyl)-pyridin-4-ol

2-(三氟甲基)异烟酸置于tetrakis(Acetonitrile)Copper(I)Tetrafluoroborate,Sodium Perborate Tetrahydrate,Lithium Perchlorate,Sodium Fluoride,N-氟代双苯磺酰胺体系中,用 四氢呋喃,水,乙腈 用作溶剂,化学反应 7.0H,反应生成2-三氟甲基-4-羟基吡啶
参考文献:铜电荷转移催化使(杂)芳基酸脱羧硼化和交叉偶联
标题:铜电荷转移催化使(杂)芳基酸脱羧硼化和交叉偶联
摘要:我们报告了一种用于芳基硼酸酯合成的铜催化策略,该策略利用光诱导配体到金属电荷转移 (Lmct) 将(杂)芳基酸转化为适合环境温度硼化的芳基自由基.这种近紫外过程在温和条件下发生,不需要对天然酸进行预功能化,并且广泛适用于各种芳基,杂芳基和药物底物.我们还报告了一种用于脱羧交叉偶联的一锅程序,该程序将催化 Lmct 硼酸化和钯催化的 Suzuki-Miyaura 芳基化,乙烯基化或与有机溴化物的烷基化结合起来,以获得一系列增值产品.通过开发异选择性双脱羧 C(Sp 2 )-c(Sp 2)偶联序列,铜催化的两种不同酸(包括药物底物)的 Lmct 硼化和卤化过程与随后的 Suzuki-Miyaura 交叉偶联配对.
Doi:10.1021/jacs.2C01630

专利信息

专利号:US-12304912-B2
优先权日:2020-07-28
标 题 :Fused bicyclic RAF inhibitors and methods for use thereof
发明人：BELFIELD ANDREW; JONES CLIFFORD DAVID; MARGATHE JEAN-FRANÇOIS; COLLETTO CHIARA
权利人:JAZZ PHARMACEUTICALS IRELAND LTD
摘要:The present disclosure generally relates to improved synthesis of fused bicyclic Raf inhibitors of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof. The disclosure also relates to method of using the compound of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, for treating diseases such as cancer, including colorectal cancer.