10.1016/j.tetlet.2006.04.096
This research article details the one-pot synthesis of quinazolinone derivatives, which are important fused heterocycles with a range of biological activities such as anti-cancer, anti-inflammatory, and anti-malarial properties. The study aimed to develop an efficient method for the synthesis of 4(3H)-quinazolinones using anthranilic acid, trialkyl orthoformate, and amines in the presence of catalysts lanthanum(III) nitrate hexahydrate [La(NO3)3·6H2O] or p-toluenesulfonic acid (PTSA) under solvent-free conditions. The process was found to be simple, efficient, and environmentally friendly, yielding 4(3H)-quinazolinones in a single step with mild catalysts, fast reaction times (5–15 minutes), and excellent yields (82–98%). The chemicals used in the process include anthranilic acid, various substituted alkyl and aryl amines, trimethyl or triethyl orthoformate, and the catalysts La(NO3)3·6H2O or PTSA. The conclusions highlight the advantages of the protocol, such as the solvent-free conditions, simplicity of the experimental procedure, and the high yields obtained, making it a practical alternative to previous methods with environmental and economic considerations.