| 摘要 |
A kanamycin derivative of the formula IV <IMAGE> is prepared by reacting 6-carbobenzoxykanamycin A with, for example, benzaldehyde to give the corresponding Schiff's base which, after reaction with the N-hydroxy-5-norbornene-2,3-dicarboximide ester of L- gamma -benzyloxycarbonylaminoalpha -hydroxybutyric acid and subsequent hydrogenation of the residue in situ, yields the compound IV. The process is more selective than known processes in respect of the acylation of the 1-amino group. The compound has excellent antibacterial activity exceeding that of kanamycin A. |
