http://rdf.ncbi.nlm.nih.gov/pubchem/patent/SE-7908850-L

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filingDate 1979-10-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_adeddf8f820514cec10a80eb79f0aeab
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publicationDate 1980-05-12-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber SE-7908850-L
titleOfInvention PREPARATION OF A SELECTIVE PROTECTED N-ACYLATED DERIVATIVE OF AN AMINOGLYCOSIDE ANTIBIOTIC
abstract Aminoglycosidic antibiotic comprising a 6-0-(3''-aminoglycosyl)-2-deoxystreptamine optionally having a 4-0-(aminogycosyl) group, such as kanamycins, gentamicins, sisomicin, forms reversible complex with zinc cations by association of the zinc cations with some pairs of aminohydroxyl groups in the aminoglycoside, and the zinc-complexed amino groups are blocked from acylation. Reaction of this zinc complex with an acylation reagent having an amino-blocking acyl group brings about acylation of the non-complexed amino groups to give an N-acylated zinc complex, namely a complex of zinc cation with an N-acylated aminoglycosidic antibiotic derivative. Removal of zinc cations from N-acylated zinc complex yields a partially N-acylated aminoglycosidic antibiotic where 1- and 3''-amino groups are unprotected but all other amino groups protected with acyl group. Further reaction of this partially N-acylated product with a certain alkanoic acid or N-formyl-imidazole results in preferential acylation of 3''-amino group without 1-amino group being acylated, affording a 1-N-unprotected and other N-fully-protected derivative of the aminoglycosidic antibiotic which is valuable to be 1-N-acylated with alpha -hydroxy- omega -aminoalkanoic acid for high-yield production of known semi-synthetic 1-N-( alpha -hydroxy- omega -aminoalkanoyl)-aminoglycosidic antibiotic.
priorityDate 1978-11-11-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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Total number of triples: 25.