Departamento de Química Orgánica, Facultad de Química, Universidad Complutense, 28040 Madrid, Spain.
Chemistry. 2010 Feb 1;16(5):1592-600. doi: 10.1002/chem.200902685.
A novel approach for the synthesis of macrocyclic bis-beta-lactams based on the Cu-catalyzed alkyne-azide cycloaddition (CuAAC) is reported. The procedure is general and allows access to a full range of diastereomerically or enantiomerically pure macrocyclic cavities in good yields. The incorporation of chiral oxazolidinone fragments at C3 in the beta-lactam rings allows the total enantiocontrol of the process.
本文报道了一种基于铜催化的炔烃-叠氮环加成（CuAAC）反应合成大环双β-内酰胺的新方法。该方法具有通用性，可以高产率获得各种非对映异构体纯或对映异构体纯的大环空腔。在β-内酰胺环的 C3 位引入手性恶唑烷酮片段可以实现整个过程的完全对映控制。
