| 摘要 |
The invention relates to a method for the preparation of isepamycin, semi-synthetic antibiotic of the group of the aminoglucosides. By the method, isepamycin is produced by using a widespread accessible protection reagent, at minimum consumption of S-isoserine and a simplified control scheme. The method includes the interaction between gentamycin B and zinc pivaloate, selective protection of 3,6'-aminogroups of gentamycin B in its inter-reaction with benzyloxy carbonyloxy-succinamide in a dimethylsulphoxide medium, in the presence of zinc pivaloate at room temperature and continuous agitation. Then 25% ammonia is added, the mixture is diluted in water and the pH is adjusted to 7.5 by means of 2M phosphate buffer. The produced 3,6'-di-N-benzyloxycarbonylgentamycin B is purified by an ion-exchange agent on weak cationite, the product is eluated by 2% ammonia, the eluate is acylated with 1.2-1.5 ml/mol N-phormylisoserine. To the mixture, 25% ammonia is added, is diluted with water and is filtered. The filtrate produced containing 1-N-(S-beta-phormylamino-alpha-hydroxypropionyl)-3,6'-di-N-benzylo xycarbonyl gentamycin B is hydrated in the presence of 5% palladium as catalyst on a carbon, after which the catalyst is filtered, and the formyl group of the isoserine residue is subjected to alkaline hydrolysis. 2 claims
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