α-亚甲基-γ-丁内酰胺衍生物的合成进展

The Synthesis of α-Methylene-γ-lactam Derivatives

α-亚甲基-γ-丁内酰胺衍生物具有细胞毒性、抗肿瘤等生理活性,有关这些化合物的合成方法一直是人们感兴趣的课题之一。本文拟就(1)含必要官能团的开链前体的成环反应,(2)现成的γ-丁内酰胺的α-亚甲基化反应等两个方面对α-亚甲基-γ-丁内酰胺的合成方法进行综述。

The synthesis of α- methylene - γ - lactam derivatives is an interesting subject owing to the biological activities such as cytotoxicity, antitumority.etc. The present review summarizes the methods for the preparation of α - methylene - γ - lactams, which are classified into groups: (1) construction of the α - methylene - γ - lactam ring from acyclic precursors bearing all necessary functional groups and (2) introduction of α -methylene group on to a preformed lactam ring.