Laboratory of Synthetic Chemistry, SAIC-Frederick, Inc., National Cancer Institute at Frederick, 1050 Boyles Street, Frederick, Maryland 21702, USA.
J Org Chem. 2011 May 6;76(9):3527-30. doi: 10.1021/jo102558u. Epub 2011 Mar 31.
Monocyclic as well as fused bicyclic systems with a nitrogen 10 atom at the bridgehead, including indolizidines and quinolizidines, can be prepared in four steps from N-Boc β-lactams. These easily prepared, highly robust, and flexible building blocks allow the incorporation of chirality and structural diversity, rendering the method feasible for diversity- as well as target-oriented synthesis.
单环以及稠合双环系统,包括吲哚里嗪和喹诺里嗪,都可以通过 N-Bocβ-内酰胺四步制备得到,桥头上有一个氮 10 原子。这些易于制备、高度稳定且灵活的构建块允许引入手性和结构多样性,使得该方法可用于多样性导向和基于靶点的合成。