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β-内酰胺因有四元环结构,又是某些抗生素的母体,它的合成一直受到有机化学家的注意。1980年Melillo等用DCC为缩合剂由β-氨基酸脱水直接合成了β-内酰胺,1981年Kobayashi等报告了以Ph_3P—(PyS)_2为缩水剂由β-氨基酸合成β-内酰胺,1984年我们用2-氯吡啶盐为脱水剂成功的得到了β-内酰胺。本文报道在三聚氯氰及二甲基甲酰胺存在下使β-氨基酸环合成β-内酰胺的新方法。用这种新方法共合成了六种β-内酰胺Ⅱ_(a-f)。其特点是反应在温和的条件下进行,分离产品比较容易,产率约为56—90％左右,此法比较方便,尚未见文献报道。
Because of its four-membered ring structure, β-lactam is also the mother of some antibiotics, and its synthesis has attracted the attention of organic chemists. In 1980, Melillo et al. Directly synthesized β-lactam from β-amino acid dehydration by using DCC as condensing agent. In 1981, Kobayashi et al. Reported the synthesis of β-lactam from β-amino acid with Ph_3P- (PyS) _2 as a shrinkage agent. We successfully obtained β-lactam with 2-chloropyridine salt as dehydrating agent. This paper reports a new method of cyclization of β-amino acids to β-lactams in the presence of cyanuric chloride and dimethylformamide. A total of six β-lactams Ⅱ_ (a-f) were synthesized by this new method. It is characterized by the reaction under mild conditions, the separation of products is relatively easy, the yield of about 56-90%, this method is more convenient and has not been reported in the literature.