Fluorination of 2-aminopyridines and pyridin-2(1 H)-ones in the presence of Selectfluor, water, and chloroform under mild conditions has been realized. This method gives fluorinated pyridines in good to high yields… Click to show full abstract
Fluorination of 2-aminopyridines and pyridin-2(1 H)-ones in the presence of Selectfluor, water, and chloroform under mild conditions has been realized. This method gives fluorinated pyridines in good to high yields with high regioselectivities. The electron-deficient pyridine system is activated by an amino or hydroxyl group at C2. The regioselectivity of the fluorination reaction is strongly dependent upon the substituent pattern in the 2-aminopyridine or pyridin-2(1 H)-one. The transformation of the 3-fluoro-substituted pyridine derivative into fluorinated zolimidine was achieved as well.
               
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