本文发展了一种制备胍基取代氨基糖苷衍生物的新方法。用游离胍与苄氧羰酰基保护的氨基糖苷反应,可以高收率地得到胍羰基取代产物。反应中分离得到了甲氧羰酰基取代的中间体,并对反应机理进行了推测。应用这种方法,成功制备了六个氨基全部和部分衍生的胍甲酰基氨基糖苷类衍生物。 In this paper, a new method of preparing guanidino substituted aminoglycoside derivatives has been developed. The reaction of guanidinocarbonyl-protected aminoglycosides with free guanidines gave the guanidine carbonyl substitution products in good yields. The reaction was isolated methoxycarboxyl substituted intermediates, and the reaction mechanism was speculated. Using this method, six wholly and partially derivatised guanidinoglycoside derivatives were successfully prepared.