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Direct benzylic functionalization of pyridines: Palladium-catalyzed mono-alpha-arylation of alpha-(2-pyridinyl)acetates with heteroaryl halides
Herein, we report a Pd-catalyzed mono-alpha-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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Reference£º
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem