A Two-Step Procedure for the Overall Transamidation of 8-Aminoquinoline Amides Proceeding via the Intermediate <i>N</i>-Acyl-Boc-Carbamates
作者:Oscar Verho、Monireh Pourghasemi Lati、Michael Oschmann
DOI:10.1021/acs.joc.8b00174
日期:2018.4.20
In this protocol, the 8-aminoquinoline amides were first treated with Boc2O and DMAP to form the corresponding N-acyl-Boc-carbamates, which were found to be sufficiently reactive to undergo subsequent aminolysis with different amines in the absence of any additional reagents or catalysts. To demonstrate the utility of this approach, it was applied on a number of 8-aminoquinoline amides from the recent
在本文中,已经探索了实现8-氨基喹啉酰胺的整体转氨基的两步策略。在该方案中,首先将8-氨基喹啉酰胺用Boc 2 O和DMAP处理,以形成相应的N-酰基-Boc-氨基甲酸酯,发现它们具有足够的反应活性,可以在没有任何其他添加剂的情况下用不同的胺进行后续的氨解。试剂或催化剂。为了证明这种方法的实用性,将其应用于最新的C–H官能化文献中的多种8-氨基喹啉酰胺中,从而能够以高产率或高产率获得一系列精细的酰胺衍生物。