Bioorganische Chemie, Institut für Chemie, Universität Hohenheim, Stuttgart, Germany.
Org Biomol Chem. 2012 May 21;10(19):3899-905. doi: 10.1039/c2ob06963f. Epub 2012 Apr 12.
Cu(I)-catalyzed reaction of o-bromobenzaldehydes with β-ketoesters using Cs(2)CO(3) as a base and 2-picolinic acid as an additive proceeds under mild conditions and gives access to substituted naphthalenes in a single step with yields ranging from 71 to 86%. The new annulation process relies on a domino Knoevenagel condensation/C-arylation/1,2-addition/carboxylic acid cleavage. The annulation can also be achieved with o-iodobenzaldehyde.
在温和条件下，使用 Cs(2)CO(3)作为碱和 2-吡啶甲酸作为添加剂，Cu(I)催化邻溴苯甲醛与β-酮酯的反应，可以一步法得到取代的萘，并获得 71%至 86%的产率。这个新的环化过程依赖于多步 Knoevenagel 缩合/C-芳基化/1,2-加成/羧酸裂解。邻碘苯甲醛也可以实现环化。
