作者:Olavi Loog、Uno Mäeorg、Ulf Ragnarsson
DOI:10.1055/s-2000-7600
日期:——
Smooth monoarylation of two triprotected hydrazine reagents under mild conditions has been accomplished using triarylbismuthanes in the presence of copper acetate and amine to give products 3 and 6 in excellent yield. Arylation on N 2 after selective deprotection of derivatives with alkyl or aryl substituents on N 1, resulting in compounds 8 and 9, is also demonstrated. Furthermore, other products derived from these reagents with free N-alkyl and N-aryl functions undergo the same reaction to give substances such as 10 and 11. As a result, the scope of the original hydrazine reagents has been further extended. A few reference compounds have also been prepared directly from phenylhydrazine.
在温和的条件下,使用三芳基铋烷在醋酸铜和胺的存在下完成了两种三保护肼试剂的平滑单芳基化反应,得到了产率极高的产物 3 和 6。在对 N 1 上带有烷基或芳基取代基的衍生物进行选择性脱保护后,N 2 上的芳基化反应也得到了化合物 8 和 9。此外,由这些试剂衍生出的具有游离 N-烷基和 N-芳基官能团的其他产物也会发生同样的反应,生成 10 和 11 等物质。因此,原始肼试剂的应用范围得到了进一步扩展。一些参考化合物也是直接从苯肼中制备出来的。