Azaarenes are unique scaffolds that are frequently found in pharmaceuticals. Herein we have summarized the recent synthetic available methods in C–H functionalization of methylazaarenes from 2010 to 2020. Multiple approaches involving halogenation, alkylation via different methods, alkenylation, oxidative functionalization, and cyclization of the methylazaarenes will be discussed in this review.
Keywords: Azaarenes, pharmaceutical, C-H functionalization, alkenylation, oxidative, cyclization.