Herein,we report a Pd-catalyzedmono- α-arylationreactionforpyridinebenzylicfunctionalization.This approach serves as an efficient altative 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