63770-47-8Relevant articles and documents
Method for synthesizing arab League Beica starbeica star and
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Paragraph 0078, (2017/01/19)
The present invention relates to a method for synthesizing dibekacin and arbekacin. The method comprises: using kanamycin B as an initial raw material, protecting five amino groups of the kanamycin B by using t-butyloxycarboryl, protecting hydroxyl of positions 4''and 6'' by aldol condensation, eliminating, in the presence of 2,4,5-triiodo-imidazol, triphenylphosphine, and imidazole, hydroxyl of positions 3' and 4' to form a double bond, removing the protection of the amino groups and the hydroxyl in a hydrochloric methanol solution, and performing catalytic hydrogenation to obtain dibekacin; and using 3',4'-didanosine-3', 4'-didehydro-kanamycin B as a raw material, protecting all the amino groups and hydroxyl by using trimethylsilyl acetate, acylating an amino group of a position 1 by using synthesized active ester, removing the protected groups by sequentially using hydrochloric acid and hydrazine hydrate, and finally, performing catalytic hydrogenation to obtain arbekacin. The synthesizing method is simple in operation, high in yield, environmentally-friendly, low in production cost, and beneficial to industrial production.