On June, 7^th, 2023, Professor Li Yizhou group at the School of Pharmaceutical Science of Chongqing University published an article on Chinese Chemical Letters entitled "Antimony salt-promoted cyclization facilitating on-DNA syntheses of dihydroquinazolinone derivatives and its applications ".

Dihydroquinazolinone (DHQ) is an important nitrogen-containing heterocycle, found in a variety of bioactive molecules with pharmacological properties ranging from antitumor and antimicrobial properties. We here describe a mild, rapid synthetic protocol to form on-DNA DHQ heterocycle featured with antimony salt-promoted cyclization. Under the conditions we developed, high conversions were mostly achieved for different aldehyde (isatin) substrates, and o-aminobenzamide substrates. On-DNA synthesized DHQ can be directly converted to quinazolinones by oxidation to achieve heterogeneous conversions without any purification. Most notably, we applied the reaction to DNA-compatible macrocyclization and successfully synthesized macrocyclic peptide compounds chimeric with drug-like scaffold DHQ, which provides new ideas for discovery of DNA-encoded macrocyclic peptide compounds.