Four-Component Cyclization of Naphthol/Thionaphthol/Naphthylamine, Formaldehyde, and DBU in Water

J Org Chem. 2022 Nov 4;87(21):13819-13827. doi: 10.1021/acs.joc.2c01532. Epub 2022 Oct 12.

Abstract

A practical and environmentally benign cascade multicomponent condensation of naphthol/thionaphthol/naphthylamine, formaldehyde, and DBU in water without any catalysts has been achieved. A wide variety of dihydrooxazine, dihydrothiazine, and tetrahydrobenzoquinazoline derivatives N-substituted with a tether bearing a caprolactam unit were afforded in moderate to good yields. The advantages of being cost-effective, metal-free, and easily handled and the use of water as medium made this protocol conform with the principle of green synthesis.