本文报道了一种环境友好的电化学方法,该方法利用俘获作用和离域作用产生氮中心自由基(NCR)。通过改变电极材料的反应参数和原料溶解度,脱芳香化使选择性脱氢的CN与NN键形成反应成为可能。因此,吡啶[1,2- a ]苯并咪唑和四芳基肼构架是通过具有广泛普遍性的可持续的无过渡金属和外源氧化剂的策略制备的。生物活性测定表明,吡啶并[1,2- a ]苯并咪唑类化合物具有抗微生物活性和对人类癌细胞的细胞毒性。化合物21具有良好的光化学性质,具有大的斯托克斯位移(约130 nm),并成功应用于亚细胞成像。初步的机理研究和密度泛函理论(DFT)计算揭示了可能的反应途径。
本文报道了一种环境友好的电化学方法,该方法利用俘获作用和离域作用产生氮中心自由基(NCR)。通过改变电极材料的反应参数和原料溶解度,脱芳香化使选择性脱氢的CN与NN键形成反应成为可能。因此,吡啶[1,2- a ]苯并咪唑和四芳基肼构架是通过具有广泛普遍性的可持续的无过渡金属和外源氧化剂的策略制备的。生物活性测定表明,吡啶并[1,2- a ]苯并咪唑类化合物具有抗微生物活性和对人类癌细胞的细胞毒性。化合物21具有良好的光化学性质,具有大的斯托克斯位移(约130 nm),并成功应用于亚细胞成像。初步的机理研究和密度泛函理论(DFT)计算揭示了可能的反应途径。
readily available N-(2-pyridyl)anilines and commercially available α-Cl ketones through iridium-catalyzed C–H activation and cyclization is reported here. As a complementary approach to the conventional strategies for indole synthesis, the transformation exhibits powerful reactivity, tolerates a large number of functional groups, and proceeds with good to excellent yields undermildconditions, providing
A compound represented by formula (I) or an isomer or a pharmaceutically acceptable salt thereof. The present invention also relates to an application of the same in preparing a drug for treating a disease related to a PGI2 receptor.
Indole is a ubiquitous structural motif with important applications in many areas of chemistry. Given this, a simple and efficient Ru(II)-catalyzed synthesis of indole via intermolecular annulation of N-aryl-2-aminopyridines and sulfoxonium ylides was proposed and accomplished. Excellent selectivity and good functional group tolerance of this transformation were observed. This protocol provides easy
The first radiosynthesis of 2-amino-5-[<sup>18</sup>F]fluoropyridines <i>via</i> a “minimalist” radiofluorination/palladium-catalyzed amination sequence from anisyl(2-bromopyridinyl)iodonium triflate
synthesis of 2-amino-5-[18F]fluoropyridines was achieved in 8-85% yields by palladium-catalyzed reaction of 2-bromo-5-[18F]fluoropyridine with piperidine, dimethylamine, butylamine, methylpiperazine, benzylamine, aniline and 3-aminopyridine. 2-Bromo-5-[18F]fluoropyridine was obtained by radiofluorination of anisyl(2-bromopyridinyl-5)iodonium triflate (88% yield). The radiofluorination step was performed
Metal-free directed C−H borylation of 2-(N-methylanilino)-5-fluoropyridines and 2-benzyl-5-fluoropyridines
作者:Gaorong Wu、Xiaobo Xu、Shuai Wang、Lu Chen、Binghan Pang、Tao Ma、Yafei Ji
DOI:10.1016/j.cclet.2021.09.081
日期:2022.4
A novel method for metal-free C−Hborylation of 2-(N-methylanilino)-5-fluoropyridines and 2-benzyl-5-fluoropyridines has been reported. The 5-fluoropyridine directedborylation reaction exhibited high efficiency and site exclusivity. The useful protocol could be executed on a gram-scale easily and the borylated products showed good derivatization applications. Moreover, the practicality of the strategy