Development of a New Synthetic Method to Synthesize Quinazolinone Derivatives

Summary
In multicomponent coupling reaction, three or more components react in a single flask to produce a single product and is often used in drug discovery research. For example, a biologically active quinazolinone derivative can be synthesized by adding an oxidant to three components (isatoic anhydride, benzaldehyde, and amine) in an organic solvent. However, since it requires a large amount of highly toxic oxidants and the preparation of benzaldehyde from alcohol, the development of a catalytic synthesis method with less environmental impact is warranted.
The group has succeeded in developing a new environmentally-friendly, multi-component coupling reaction for the synthesis of quinazolinones using water as a solvent and a water-soluble palladium catalyst. By adding a palladium catalyst to the above-mentioned three components using water as the solvent, benzyl alcohol, which has low reactivity, can be used directly in the multicomponent coupling reaction, enabling more efficient synthesis of quinazolinone derivatives.