Pd II ‐Catalyzed γ ‐C(sp ³ )–H (Hetero)Arylation of Ketones Using Acetohydrazide As The Transient Directing Group

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Pd(II)‐catalyzed γ ‐C(sp 3 )–H (hetero)arylation of aliphatic ketones is developed using acetohydrazide as the transient directing group (TDG). The reaction is facilitated by a crucial 2‐pyridone ligand via the 5,6‐membered fused palladacycle intermediate, enabling the smooth γ ‐C(sp 3 )–H (hetero)arylation of various aliphatic ketones. The reaction demonstrated tolerance to different functional groups of aryl iodides, and compatibility with various pyridinyl or quinolinyl iodides. Furthermore, regioselectivity of γ ‐C(sp 3 )–H arylation with current reaction conditions was compared with previous studies for the challenging substrate pentan‐2‐one.