3557-59-3Relevant academic research and scientific papers
Direct C-H Functionalization of Pyridine via a Transient Activator Strategy: Synthesis of 2,6-Diarylpyridines
Zeng, Yang,Zhang, Chunchun,Yin, Changzhen,Sun, Maoshen,Fu, Haiyan,Zheng, Xueli,Yuan, Maolin,Li, Ruixiang,Chen, Hua
, p. 1970 - 1973 (2017)
A Pd-catalyzed highly selective direct diarylation of pyridines has been developed using a transient activator strategy. Both (MeO)2SO2 and Cu2O are required for this transformation. The in situ generated N-methylpyridinium salt can be arylated at both 2- and 6-positions under the cooperative Pd/Cu catalysis. A subsequent N-demethylation then gives the 2,6-diarylpyridines. This protocol provides a novel synthetic route for the symmetric 2,6-diarylpyridines.
Method for double carbon-hydrogen activation and arylation of pyridine compounds
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Paragraph 0062; 0063; 0064; 0065; 0066; 0079; 0080; 0081-008, (2017/04/21)
The invention discloses a method for double carbon-hydrogen activation and arylation of pyridine compounds, and belongs to the field of methodology of organic synthesis. The method comprises the following steps: mixing a palladium source, a phosphine ligand, a copper salt or an oxide of copper, an alkali and aryl halide, placing the mixture in a nitrogen gas environment, then adding an additive, 4-substituted pyridine and a solvent, and carrying out a heating reaction, to obtain a C2-site and C6-site double aryl substituted pyridine compounds through a carbon-hydrogen activation mechanism, wherein a substituent group of 4-substituted pyridine is any one of hydrogen, alkyl and aryl. The method has the advantages of wide application range, simple operation steps, no need of pre-activation of a pyridine ring, and no need of introduction of a guiding group, and extremely high atomic economy and practicability.
