138761-51-0Relevant articles and documents
A Convenient Late-Stage Fluorination of Pyridylic C?H Bonds with N-Fluorobenzenesulfonimide
Meanwell, Michael,Nodwell, Matthew B.,Martin, Rainer E.,Britton, Robert
, p. 13244 - 13248 (2016)
Pyridine features prominently in pharmaceuticals and drug leads, and methods to selectively manipulate pyridine basicity or metabolic stability are highly sought after. A robust, metal-free direct fluorination of unactivated pyridylic C?H bonds was developed. This convenient reaction shows high functional-group tolerance and offers complimentary selectivity to existing C?H fluorination strategies. Importantly, this late-stage pyridylic C?H fluorination provides opportunities to rationally modulate the basicity, lipophilicity, and metabolic stability of alkylpyridine drugs.