| 摘要 |
<p>NEW MATERIAL:The compound of formula I and its acid addition salt. USE:Semi-synthesized aminoglycoside antibiotic substance. PROCESS:The amino groups or methylamino groups at the 1, 2'- and 6'-positions of the istamycin A0 of formula II are protected with alkoxycarbonyl groups, etc. at the same time, to obtain the compound of formula III (R is univalent amino-protecting group), which is acylated with glycine or its reactive derivative wherein the amino groups are protected with protecting groups different from the above amino-protecting groups, e.g. N-tert-butoxycarbonyl glycin N-hydroxysuccinimide ester, etc., in an organic solvent such as dioxane, at 40-60 deg.C, to afford the compound of formula IV (A is H; B is univalent amino-protecting group, etc.). The amino groups at the glycine segment of the compound of formula IV are exclusively and selectively eliminated, and the resulted compound is made to react with an imino ether to convert the amino group of the glycine segment to amidine group. Finally, the amino-protecting groups at the 1, 2'- and 6'-positions are eliminated to obtain the objective compound of formula I.</p> |
