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用Dane盐与不同取代的二苯甲亚胺环合,制备了11种未见报道的α-酰氨基-β-内酰胺,研究了二苯甲亚胺的取代基对成环反应的影响;用逐步回归分析方法建立了环合反应收率与二苯甲亚胺上取代基的取代常数之间的相关关系。研究表明,环合收率与二苯甲亚胺上取代基的电性效应常数σ值呈负的线性关系,与甲亚胺的 pK(?)值呈正的线性关系。利用取代基的σ值和甲亚胺的pK(?)值可以预测同系列化合物成环反应活性的相对高低。
Eleven newly reported α-amido-β-lactams were prepared by cyclodehydrogenation of dane salts with different substituted benzidine. The effects of substituents of benzidine on the cyclization reaction were investigated. A stepwise regression analysis was used to establish the correlation between the yield of the cyclization reaction and the substitution constant of the substituents on the benzidine. The results show that the ring closure yield has a negative linear relationship with the σ value of the substituent on the benzidine, and a positive linear relationship with the pK (?) Value of the azomethine. Using the σ value of the substituent and the pK (?) Value of azomethine, the relative degree of cyclization activity of the same series of compounds can be predicted.