Ligand-free iron-catalyzed benzylic C (sp3)-H amination of methylarenes with: N -fluorobenzenesulfonimide
Direct conversion of cheap methylarenes to benzylic amines, which are essential structural units of important drugs, is of great significance. However, the known methodologies suffer from the requirement of noble metal catalysts, heavy metal residues or s
Bao, Fengyu,Cao, Yuanbo,Liu, Wenbo,Zhu, Junhao
p. 27892 - 27895
(2019/09/30)
Direct amination of benzyl C-H of methyl aromatic compound under iron catalysis
The invention provides a direct amination of benzyl C-H of a methyl aromatic compound under iron catalysis. The method comprises the following steps: the methyl aromatic compound is used as a raw material, an iron compound is used as a catalyst, o-dichlor
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Paragraph 0017
(2019/07/29)
Late-Stage Functionalization of Arylacetic Acids by Photoredox-Catalyzed Decarboxylative Carbon–Heteroatom Bond Formation
The rapid transformation of pharmaceuticals and agrochemicals enables access to unexplored chemical space and thus has accelerated the discovery of novel bioactive molecules. Because arylacetic acids are regarded as key structures in bioactive compounds, new transformations of these structures could contribute to drug/agrochemical discovery and chemical biology. This work reports carbon–nitrogen and carbon–oxygen bond formation through the photoredox-catalyzed decarboxylation of arylacetic acids. The reaction shows good functional group compatibility without pre-activation of the nitrogen- or oxygen-based coupling partners. Under similar reaction conditions, carbon–chlorine bond formation was also feasible. This efficient derivatization of arylacetic acids makes it possible to synthesize pharmaceutical analogues and bioconjugates of pharmaceuticals and natural products.
Highly regioselective copper-catalyzed benzylic C-H amination by N-fluorobenzenesulfonimide
Primary target: A practical and effective copper-catalyzed amination strategy for synthesizing various benzylic amines from benzylic hydrocarbons is described (see scheme; DCE=1,2-dichloroethane). Xylene substrates can undergo diamination reactions using this method. The remarkable preference for primary over secondary benzylic C-H bonds has been observed for the first time. Copyright