Outline
DOI: 10.1021/acs.orglett.6c04364 ISSN: 1523-7060
Cascade Cyclization of 2-Aryl Quinazolinones with 2,2-Difluorovinyl Tosylate: A One-Pot Formal [4 + 2] Approach to Fluorinated Fused Quinazolinones
Xiangjian Zhong, Xuemei Xiao, Jiahao Yang, Zhifei He, Cuiyan Zeng, Gaorong WuAbstract
Herein, a novel [4 + 2] cascade cyclization strategy is developed to construct fluorinated fused quinazolinones via tandem C–C/C–N bond formation in the green solvent PEG-400. This protocol features good functional group tolerance, high efficiency and operational simplicity. Furthermore, the resulting fluorinated heterocycles represent new chemical entities, which may provide valuable insights for drug discovery.
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