Ye Chenghao, Kou Xuezhen, Xia Jingzhao, Yang Guoqiang, Kong Li, Wei Quhao, Zhang Wanbin
Shanghai Key Laboratory for Molecular Engineering of Chiral Drugs, School of Chemistry and Chemical Engineering, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai, 200240, China.
6th People's Hospital South Campus, Shanghai Jiao Tong University, 6600 Nanfeng Hwy, Shanghai, 200233, China.
Chem Asian J. 2018 May 30. doi: 10.1002/asia.201800646.
A Pd -catalyzed oxidative tandem cyclization was developed for the construction of fused 5,6-bicyclic N, O-heterocycles. This reaction was enabled by the combined use of a 3-methylpyridine ligand and pentafluorobenzoic acid additive. A range of heterocyclic products with different substituents could be prepared in moderate to good yields via this methodology. Several transformations, including a scaled-up preparation of product 2 a, were also carried out showing the good applicability of our methodology.
开发了一种钯催化的氧化串联环化反应来构建稠合的5,6-双环N,O-杂环。该反应通过3-甲基吡啶配体和五氟苯甲酸添加剂的联合使用得以实现。通过该方法可以以中等至良好的产率制备一系列具有不同取代基的杂环产物。还进行了几种转化反应,包括产物2a的放大制备,展示了我们方法的良好适用性。