Triflimide-Promoted Nucleophilic C-Arylation Of Halopurines To Access N-7-Substituted Purine Biaryls

Functionalized nucleobases are utilized in a wide range of fields; therefore, the development of new synthesis methods is essential for their continued application. With respect to the C-6-arylation of halopurines, which possess a substituent at the N-7-position, only a small number of successful cases have been reported, which is predominately a result of large steric hinderance effects. Herein, we report efficient and metal-free C-6-arylations and SNAr reactions of N-7-substituted chloropurines in aromatic and heteroatom nucleophiles promoted by trillimide (Tf2NH) in fluoroalcohol.