Direct, efficient, solvent-free synthesis of 2-aryl-1,2,3,4-tetrahydroquinazolines

Abstract

2-Aryl-1,2,3,4-tetrahydroquinazolines are synthesised by direct reaction of 2-aminobenzylamine and benzaldehyde derivatives by mixing of the reagents either neat, or as an aqueous slurry. Excellent conversion of starting materials is achieved and no catalysts, derivatisation or auxiliary reagents are required to effect the conversion. Where reaction is sluggish or extent of conversion poor, application of gentle heating to achieve a melt phase results in rapid and clean conversion to the desired tetrahydroquinazoline product.