| Direct benzylic functionalization of pyridines:Palladium-catalyzed mono-α-arylation of α-(2-pyridinyl)acetates with heteroaryl halides |
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| 作者姓名： | Chaochao Jin Kun Xu Xiao Fan Changyao Liu Jiajing Tan |
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| 作者单位： | Department of Organic Chemistry, College of Chemistry, Beijing Advanced Innovation Center for Soft Matter Science and Engineering, Beijing University of Chemical Technology, Beijing 100029, China;
; College of Chemistry and Pharmaceutical Engineering, Nanyang Normal University, Nanyang 473061, China;
; School of Food and Chemical Engineering, Beijing Technology and Business University, Beijing 100048, China |
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| 基金项目： | Tan is grateful to the support by the National Natural Science Foundation of China (No. 21702013), Beijing Natural Science Foundation (No. 2184115) and the Fundamental Research Funds from the Central Universities (Nos. XK1802-6, buctrc201721) in Beijing University of Chemical Technology. |
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| 摘 要： | Herein,we report a Pd-catalyzed mono-a-arylation reaction for pyridine benzylic functionalization.This approach serves as an efficient alternative to synthesize di-heteroaryl acetates in good yields and selectivities.Moreover,the method is applicable to heteroa ryl substrate combinations,and exhibits great functional group tolerance.A streamlined protocol also enables the rapid synthesis of diheteroaryl ketones.The synthetic value was also demonstrated by scale-up experiments.
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| 关 键 词： | α-Arylation Palladium HETEROCYCLES PYRIDINES CROSS-COUPLING |
| 收稿时间： | 9 April 2019 |
Direct benzylic functionalization of pyridines: Palladiumcatalyzed mono-α-arylation of α-(2-pyridinyl)acetates with heteroaryl halides |
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| Chaochao Jin,Kun Xu,Xiao Fan,Changyao Liu,Jiajing Tan.Direct benzylic functionalization of pyridines: Palladiumcatalyzed mono-α-arylation of α-(2-pyridinyl)acetates with heteroaryl halides[J].Chinese Chemical Letters,2020,31(1):91-94. |
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| Authors: | Chaochao Jin Kun Xu Xiao Fan Changyao Liu Jiajing Tan |
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| Institution: | Department of Organic Chemistry, College of Chemistry, Beijing Advanced Innovation Center for Soft Matter Science and Engineering, Beijing University of Chemical Technology, Beijing 100029, China; College of Chemistry and Pharmaceutical Engineering, Nanyang Normal University, Nanyang 473061, China; School of Food and Chemical Engineering, Beijing Technology and Business University, Beijing 100048, China |
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| Abstract: | Herein, we report a Pd-catalyzed mono-α-arylation reaction for pyridine benzylic functionalization. This approach serves as an efficient alternative to synthesize di-heteroaryl acetates in good yields and selectivities. Moreover, the method is applicable to heteroaryl substrate combinations, and exhibits great functional group tolerance. A streamlined protocol also enables the rapid synthesis of diheteroaryl ketones. The synthetic value was also demonstrated by scale-up experiments |
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| Keywords: | α-Arylation Palladium Heterocycles Pyridines Cross-coupling |
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