School of Chemical Engineering, Nanjing University of Science and Technology , Nanjing 210094, P. R. China.
Department of Chemistry, University of Massachusetts Boston , Boston, Massachusetts 02125, United States.
Org Lett. 2016 Nov 4;18(21):5640-5643. doi: 10.1021/acs.orglett.6b02883. Epub 2016 Oct 24.
A 2-fluoro-1,3-dicarbonyl-initiated one-pot Michael addition/[5 + 1] annulation/dehydrofluorinative aromatization reaction sequence is introduced for regioselective synthesis of di-, tri-, tetra-, and pentasubstituted pyridines as well as fused pyridines. This simple and modular synthesis is performed using readily available starting materials and under transition-metal catalyst-free conditions.
介绍了一种由 2-氟-1,3-二羰基引发的一锅法迈克尔加成/[5 + 1]环加成/去氟化芳构化反应序列,用于区域选择性合成二取代、三取代、四取代和五取代吡啶以及稠合吡啶。这种简单的模块化合成方法使用易得的起始原料,并在无过渡金属催化剂的条件下进行。