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Article Abstract
The direct functionalization of privileged heterocycles could efficiently and site-selectively functionalize pharmacophores to expedite the construction of a focused library for mapping druglike chemical space. A variety of biologically active 2-indazoles have been documented, but the direct amidation of 2-indazoles remains underdeveloped. Herein, we report the first transition metal-free 3-amidation of 2-indazoles under photoredox conditions. Employing 1,2,3,5-tetrakis(carbazol-9-yl)-4,6-dicyanobenzene (4CzIPN) as an inexpensive photocatalyst and -aminopyridinium salts as the amidyl radical sources, various 3-amidated 2-indazoles were generated (22 examples, up to 90% yield). Furthermore, we also achieved photocatalytic late-stage modification of drug molecules. This protocol may represent a feasible molecular editing strategy on privileged drug scaffolds to efficiently generate a focused library.
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