Efficient construction of a β-naphthol library under continuous flow conditions

Abstract

A β-naphthol library has been efficiently constructed utilizing a mild continuous flow procedure, relying on a tandem Friedel–Crafts reaction and starting from readily available arylacetyl chloride and alkynes. Multiple functionalized β-naphthols can be acquired within 160 s in generally high yields (up to 83%). Using an electron-rich phenylacetyl chloride derivative (4-OH- or 4-MeO-) provides spirofused triene dione as the primary product. A scale-up preparation affords a throughput of 4.70 g h⁻¹, indicating potential large-scale application. Herein, we present a rapid, reliable, and scalable method to obtain various β-naphthols in the compound library.