Scheme 1. Challenges Associated with the Synthesis of N-H–THQs and Biologically Important Targets That Can be Derived from the N-H–THQ Core Structure.

(A) General principle of the generation of secondary α-aminoalkyl radicals from N-alkyl anilines; (B) previous methodologies for the synthesis of N-H–THQ; (C) this work; and (D) numbering of the THQ scaffold and examples of biologically active THQ and quinolines.