Laboratoire de Chimie Organique, Institute of Chemistry, Biology and Innovation (CBI)-ESPCI Paris/CNRS, (UMR8231)/PSL* Research University, 10 rue Vauquelin, 75231, Paris Cedex 05, France.
Queen Mary University of London, School of Biological and Chemical Sciences, Mile End Road, London, E1 4NS, UK.
Chemistry. 2018 Jun 7;24(32):8076-8080. doi: 10.1002/chem.201800920. Epub 2018 May 14.
The synthesis of diversely substituted five-membered ring succinimide derivatives is reported featuring a direct, base-free, palladium-catalyzed asymmetric allylic alkylation. The method allows a straightforward access to the desired heterocyclic scaffold bearing an all-carbon α-quaternary stereogenic center in high yields and good to excellent enantioselectivities. To further demonstrate the synthetic utility of the method, the allylated products were further converted to various versatile chiral building blocks, including a chiral pyrrolidine and a spirocyclic derivative, using selective transformations.
本文报道了一种通过直接、无碱、钯催化的不对称烯丙基烷基化反应来合成各种取代的五元环琥珀酰亚胺衍生物的方法。该方法可以高收率和优异到极好的对映选择性直接获得含有全碳α-季碳手性中心的所需杂环骨架。为了进一步证明该方法的合成实用性,使用选择性转化,将烯丙基化产物进一步转化为各种多功能的手性构建块,包括手性吡咯烷和螺环衍生物。