A direct visible‐light mediated coupling of azaarenes with diversely functionalized alkyl carbons via organophotocatalytic sp3C‐H bond activation

Substituted azaarenes are one of the most ubiquitous moieties in natural products and drug molecules. An efficient organophotocatalytic method for direct coupling of diverse cyclic and acyclic alkyl carbons of alcohols, ethers, alkyl halides and alkanes with different azaaryl systems has been developed. It uses low loading of easily synthesizable efficient acridinium based photocatalyst and blue LED to generate highly reactive radicals on saturated hydrocarbons through sequential single electron transfer (SET) and hydrogen atom transfer (HAT) process. These in situ generated nucleophilic carbon radicals then undergo instantaneous regio‐selective coupling with azaarenes through Minisci type coupling to generate an array of important pharmacophores through sp2C‐sp3C bond formation. With inexpensive organophotocatalysts, higher yield and wide substrate scope, this method provides a greener, efficient and versatile alternative to the previously reported syntheses.