形成大环内酰胺方法的进展

Recent Progress in the Formation of Macrolactams

本文综述了近年来发展的形成大环和柄型大环内酰胺的方法及其在天然产物合成中的应用。Wasserman组用β-内酰胺的方法合成含多个氨基的大环内酰胺是此领域的一大进展。用金属原子作摸板的双倍活化法最具发展前景。

This paper reviews briefly the recent progress in the formation of macrolactamsand the application in natural macrolactam synthesis.A novel approach for the prepartion ofpolyamine macrolactam has been achieved by Wasserman group via the intramolecular ringopening of the β-lactam ring as a means of introducting a α-aminopropionic acid residue.Ametal template-driven extrusion process may be the most promising method for the doubleactivation of seco-amino acid and macrolactamization in the future.