PROCESS FOR PREPARING AMICACIN AS SULFURIC ACID ADDITION SALTS

摘要

FIELD: chemical industry. SUBSTANCE: the product: amicacin sulfate. Reagent 1: an anhydrous complex of 3,6-di-N-benzylo-xycarbonyl kanamycin A with a divalent metal, possibly "in situ". Reagent 2: sulfuric acid. Reaction conditions: reagent 1 is polysilated in anhydrous DMFA, DMSO, pyridine or hexamethylsilazane, optionally by addition of dipicolinic acid or 3-hydroxypyridine. The resulting polysilyl derivative is subjected to reaction of (a) partial hydrolysis using water or alcohol in an amount of 3.3 to 10% with respect to the solvent and there-after acylated with N-hydroxysuccinimide ester of L-(-)-alpha-benzyloxycarbonylamine- alpha-hydroxybutyric acid and (b) hydrogenolysis in water with the addition of methanol at a pH of 1-3, preferably 1.5-2. After purification on ionites and removal of the solvent, sulfuric acid is successively added to adjust a pH to 1-5, preferably 1-2 and alcohol, preferably methanol, in an amount of 20-50% preferably 25-40% of the volume of the aqueous phase. The desired product is of high purity and meets the requirements for substances used as injection solutions. The yield is 49-82% The biological activity is 723 mg/mg per dry matter. EFFECT: more efficient preparation process.