β-内酰胺类抗生素是目前最具应用价值的抗生素,其结构特征具有β-内酰胺环的基元结构,该类化合物的设计、合成和立体化学研究一直是有机合成化学研究的前沿和热点领域.二茂铁凭借其独特的结构和多样的性质,在生物和医药方面均有广泛的应用价值.因此,二茂铁修饰的β-内酰胺是一类结构新颖且具有潜在生物活性的化合物.对该类化合物的深入研究,将对新型抗生素的研发提供重要的指导意义.综述了近年来青霉烷类和头孢烯类β-内酰胺及单环类β-内酰胺这两大类含二茂铁取代的β-内酰胺衍生物的合成与生物活性的研究进展. β-lactam antibiotics are the most valuable antibiotics at present, and their structural characteristics have the basic structure of β-lactam ring. The design, synthesis and stereochemistry of these compounds have been the forefront and hotspot of organic synthesis chemistry Ferrocene has a wide range of applications in biology and medicine due to its unique structure and diverse properties.Therefore, ferrocene-modified β-lactam is a novel class of compounds with potential biological activity In-depth study of these compounds will provide important guidance for the development of new antibiotics.It is reviewed that in recent years, two classes of penicillins and cephem-β-lactams and monocyclic β-lactams Synthesis and Biological Activity of Ferrocene-Substituted β-Lactam Derivatives.