Han Jian, Wang Ning, Huang Zhi-Bin, Zhao Yingsheng, Shi Da-Qing
Key Laboratory of Organic Synthesis of Jiangsu Province, College of Chemistry, Chemical Engineering and Materials Science Soochow University, Suzhou 215123, China.
Org Biomol Chem. 2017 Jun 21;15(24):5112-5116. doi: 10.1039/c7ob01135k.
With the assistance of the same bidentate directing group, the first example of sequential, controllable C-H functionalization of β-arylethylamines at different positions for the construction of polysubstituted arenes is reported. Pd-Catalyzed highly regioselective ortho-C-H functionalization reactions of meta-aryl substituted arylethylamines are performed, including alkynylation, iodination, acetoxylation and amination, which led to a concise approach to the synthesis of polysubstituted β-arylethylamine derivatives.
在相同双齿导向基团的辅助下，报道了首例用于构建多取代芳烃的β-芳基乙胺在不同位置的顺序可控C-H官能化反应。进行了间位芳基取代的芳基乙胺的钯催化高区域选择性邻位C-H官能化反应，包括炔基化、碘化、乙酰氧基化和胺化反应，从而为多取代β-芳基乙胺衍生物的合成提供了一种简洁的方法。
