An Efficient, One-Pot Transamidation of 8-Aminoquinoline Amides Activated by Tertiary-Butyloxycarbonyl
作者:Wengang Wu、Jun Yi、Huipeng Xu、Shuangjun Li、Rongxin Yuan
DOI:10.3390/molecules24071234
日期:——
The efficient, one-pot access to the transamidation of 8-aminoquinoline (8-AQ), notorious for its harsh removal conditions, has been widely employed as an auxiliary in C–H functionalization reactions due to its strong directing ability. In this study, the facile and mild Boc protection of the corresponding 8-AQ amide was critical to activate the amide C(acyl)–N bond by twisting its geometry to lower
8-氨基喹啉(8-AQ)的高效、一锅转酰胺基化因其去除条件苛刻而臭名昭著,由于其强大的导向能力而被广泛用作C-H官能化反应的助剂。在这项研究中,相应的 8-AQ 酰胺的简单而温和的 Boc 保护对于通过扭曲其几何结构以降低酰胺共振能量来激活酰胺 C(酰基)-N 键至关重要。芳基胺和烷基胺均在一锅、用户友好的条件下进行转酰胺基化,并具有优异的产率。