Abdulla R F, Fuhr K H
J Med Chem. 1975 Jun;18(6):625-7. doi: 10.1021/jm00240a022.
The preparation and antimicrobial activity of a series of beta-lactams (3a-f) are described. These compounds were prepared from the 2+2 cycloaddition of beta,beta-disubstituted enamines with aryl isocyanates; compounds 3a-f underwent facile beta-lactam ring fission between aminal carbon atom C4 and the lactam nitrogen N1. The resisting formylacetanilide derivatives were devoid of antibiotic activity.
描述了一系列β-内酰胺(3a - f)的制备及其抗菌活性。这些化合物由β,β-二取代烯胺与芳基异氰酸酯的2 + 2环加成反应制备;化合物3a - f在氨基碳原子C4和内酰胺氮N1之间容易发生β-内酰胺环裂解。抗性甲酰乙酰苯胺衍生物没有抗生素活性。