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Updated: Aug 21, 2026

Palladium N-Heterocyclic Carbene Complexes: Synthesis from Benzimidazolium Salts and Catalytic Activity in Carbon-carbon Bond-forming Reactions
Published on: July 30, 2017
Ligand-enabled palladium-catalyzed late-stage C-H fluorination of arenes
Chitrala Teja1, Minhajul Islam1, Jagrit Grover1
1Indian Institute of Technology Bombay, Department of Chemistry Powai Mumbai 400076 India dmaiti@iitb.ac.in.
Abstract:
Fluorinated molecules play a vital role in medicinal chemistry, offering improved metabolic stability and bioavailability. Herein, we report a ligand-enabled C-H fluorination protocol enabled by palladium catalysis and a newly designed bidentate ligand. This strategy allows for regioselective fluorination of arenes and heteroarenes using Selectfluor as an electrophilic fluorine source under mild reaction conditions. The fluorination reaction proceeds efficiently, showcasing broad substrate scope and functional group tolerance. Notably, the methodology enables late-stage fluorination of a wide range of complex pharmaceuticals and biologically relevant molecules. Mechanistic investigations support a Pd(ii)/Pd(iv) catalytic pathway. Notably, we accomplished the one-step synthesis of fluorouracil under mild conditions, a significant advancement over traditional harsh multi-step protocols.
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