Shan Chao, Li Ranran, Wang Xinchao
Heze University Heze Shandong Province 274015 China
RSC Adv. 2024 Jan 15;14(4):2673-2677. doi: 10.1039/d3ra08660g. eCollection 2024 Jan 10.
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, indicating potential large-scale application. Herein, we present a rapid, reliable, and scalable method to obtain various β-naphthols in the compound library.
利用温和的连续流动程序，依靠串联傅克反应并从易得的芳基乙酰氯和炔烃出发，高效构建了一个β-萘酚文库。多种功能化的β-萘酚可在160秒内以通常较高的产率（高达83%）获得。使用富电子的苯乙酰氯衍生物（4-OH-或4-MeO-）时，主要产物为螺稠合三烯二酮。放大制备的通量为4.70 g/h，表明具有潜在的大规模应用前景。在此，我们展示了一种快速、可靠且可扩展的方法，用于在化合物文库中获得各种β-萘酚。
