Zhao Xiaojia, Zhang Jiong, Zheng Zeqin, Xu Runsheng
Department of Biology and Environment, Zhejiang A&F University, Shaoxing 311800, Zhejiang, China.
Molecules. 2016 Dec 30;22(1):53. doi: 10.3390/molecules22010053.
A tandem transformation of C-N coupling/C-H carbonylation has been developed for the synthesis of benzo-1,4-oxazepine pharmaceutically derivatives. Notably, this reaction was accomplished by various phenylamine with ally halides under carbon dioxide atmosphere employing 2-(2-dimethylamino-vinyl)-1-inden-1-olcatalyzed. Furthermore, under the optimized conditions, various benzo-1,4-oxazepine derivatives were obtained in good yields. Finally, a plausible Cu/Cu mechanism of C-N coupling/C-H carbonylation transformation was proposed.
已开发出一种用于合成苯并-1,4-恶唑并氮杂卓类药物衍生物的C-N偶联/C-H羰基化串联转化反应。值得注意的是,该反应是在二氧化碳气氛下,以2-(2-二甲基氨基乙烯基)-1-茚-1-醇为催化剂,由各种苯胺与烯丙基卤化物完成的。此外,在优化条件下,以良好的产率获得了各种苯并-1,4-恶唑并氮杂卓衍生物。最后,提出了一种合理的C-N偶联/C-H羰基化转化的铜/铜机理。