Convergent Domino Cyclization: Oxidative [3+1+1] Annulation for One-Pot Synthesis of 2-Quinoline-4,5-diaryl-oxazoles from Methyl Azaarenes, Benzoins and NH4OAc

An oxidative [3+1+1] convergent domino cyclization is disclosed. This protocol enables to get quinoline, quinoxaline, quinazolin-4(3H)-one and benzo[d]thiazole attached 2,4,5-trisubstituted oxazoles from methyl azaarenes, benzoins, and NH4OAc in the presence of iodine and molecular sieves without any metal catalyst. The reaction features wide substrate scope, good functional group tolerance, mild reaction conditions, and easily available substrates.

Automated summary

An oxidative [3+1+1] convergent domino cyclization method was developed for the efficient synthesis of various 2,4,5-trisubstituted oxazoles. This method features a wide substrate scope, mild reaction conditions, and easy availability of substrates.