Synthesis of N-Alkyl Substituted Benzimidazoquinazolinones

Aromatic N-heterocycles, especially benzimidazoquinazolinones featuring alkyl chains, hold significant pharmaceutical relevance. Here, we introduce a streamlined one-pot, 2-fold Cu-catalyzed C-N bond formation protocol for the efficient synthesis of diverse N-alkyl benzimidazoquinazolinone derivatives. This method showcases a broad substrate scope, leveraging readily accessible alkyl halides and delivers the desired cyclized products in excellent yields. Additionally, the methodology enabled the synthesis of an antitumor agent with satisfactory yield, highlighting its utility in medicinal chemistry endeavors.