jo5b02093_si_001.pdf (2.26 MB)
Synthesis of 2‑Keto(hetero)aryl Benzox(thio)azoles through Base Promoted Cyclization of 2‑Amino(thio)phenols with α,α-Dihaloketones
journal contribution
posted on 2016-01-04, 00:00 authored by Jun Jiang, Huaxu Zou, Qizhi Dong, Ruijia Wang, Linghui Lu, Yonggang Zhu, Weimin HeAn
interesting base-promoted protocol for the synthesis of 2-keto(hetero)aryl
benzox(thi)azoles has been developed. Starting from commercially available
2-amino(thio)phenols and α,α-dihaloketones, moderate to
good yields of the corresponding heterocycles can be achieved. Notably,
only EtNH2 was required as the promoter here, and the reaction
can be easily performed on a large scale.