CAS: 651-83-2; 2,3,5,6-Tetrafluoro-4-(Trifluoromethyl)Aniline

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CAS号434-64-0 八氟甲苯 | CAS号100758-21-2 benzylidene 4-t... | CAS号80850-06-2 1,2,4,5-tetrafl... | CAS号105637-41-0 4-trifluorometh... | CAS号1868-85-5 (α,α,α,2,3,5,6-... | CAS号114973-35-2 N-[2,5-difluoro... | CAS号98583-25-6 oxido-[2,3,5,6-...

📜八氟甲苯置于ammonium Hydroxide体系中,用 四氢呋喃 作为反应溶剂,化学反应 18.0H,以49%的收率获得产物4-氨基七氟甲苯
参考文献:氢键定向光催化加氢脱氟:克服电子控制
标题:氢键定向光催化加氢脱氟:克服电子控制
摘要:高度氟化的芳烃的光催化c-F功能化是一种获得功能化的多氟化芳烃的有力方法.确定氟官能度中区域选择性的决定性步骤是来自多氟化芳烃的自由基阴离子的氟化物裂解.迄今为止,区域异构体的可用性已由氟化芳烃的固有电子决定,限制了化学方法的合成用途.这项研究调查了位于战略位置的氢键具有超越c-f功能化事件的正常区域选择性的显着能力.另外观测到氟的加氢脱氟有明显的速率加速,氟可以经历分子内的氢键,与中等酸性的n-h形成5-8元循环.氢键有望不仅通过使自由基阴离子的c-F键弯曲到平面之外,而且通过通过裸氟化物的质子化增加氟化物挤出步骤的放热性,来促进断裂.最后,该方法的合成效用在快速合成抗糖尿病药物januvia所需的三氟化α-苯基乙酸衍生物的合成中得到了证明.这代表了通过脱氟策略对商业上重要的多氟化芳烃的首次合成,并且比目前的策略要短得多.最后,该方法的合成效用在快速合成抗糖尿病药物januvia所需的三
DOI:10.1021/jacs.7B06847

专利信息

专利号:WO-2015131100-A1
优先权日:2014-02-28
标题:Ligand-controlled c(sp3)-h arylation and olefination in synthesis of unnatural chiral alpha amino acids
发明人：YU JIN-QUAN
权利人:SCRIPPS RESEARCH INST
摘要:The use of ligands to tune the reactivity and selectivity of transition metal-catalysts for C(-sp3)-H bond functionalization is a central challenge in synthetic organic chemistry. Herein, we report a rare example of catalyst-controlled C(sp3)-H arylation using pyridine and quinoline derivatives: the former promotes exclusive monoarylation, whereas the latter activates the catalyst further to achieve diarylation. Successive application of these ligands enables the sequential diarylation of a methyl group in an alanine derivative with two different aryl iodides, affording a wide range of β-Ar-p-Ar ' -cc-amino acids with excellent levels of diastereoselectivity (d.r. > 20:1). Both configurations of the β-chiral center can be accessed by choosing the order in which the aryl groups are installed. The use of a quinoline derivative as a ligand also enables C(sp3)-H olefination of a protected alanine.

专利号:WO-2008074219-A1
优先权日:2006-12-20
标 题 :Chloride of 2-(6'-imdopyridyl) benzimidazole metal complex, its synthesis and its application