Visible-Light-Induced Preparation of Quinazolinones by Oxidation of Benzyl Alcohols in Water

A novel visible-light-introduced reaction for the construction of quinazolinone derivatives via radical cyclization of 2-aminobenzamides with benzyl alochols under water phase has been developed. The reaction has been achieved in high yield under mild conditions by using I-2 as photocatalyst, which is cheap, available and easy to handle. A variety of quinazolinones were obtained in yields up to 92%. It might provide a promising protocol for the synthesis of quinazolinone derivatives. Its application was performed by the synthesis of N-(2-fluoro-5-methylphenyl)-6-(2,2,2-trifluoroethoxy)pteridin-4-amine, which displayed significant inhibitory activity.

Automated summary

A novel visible-light-induced reaction for the construction of quinazolinone derivatives via radical cyclization of 2-aminobenzamides with benzyl alcohols under water phase has been developed. It achieved high yields under mild conditions using I-2 as a photocatalyst, which is cheap, available and easy to handle. This method could provide a promising protocol for the synthesis of quinazolinone derivatives.