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filingDate 1978-12-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_92b5dbdbb2968008aeb158620c8ee760
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publicationDate 1980-06-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber JP-S5581897-A
titleOfInvention Preparation of 1-n-isoseryl-or 1-n-(l-4-amino-2-hydroxybutyryl)-3',4'-dideoxykanamycin b
abstract PURPOSE: To obtain the title compound effective against various resistant bacteria, including Pseudomonas aeruginosa, in high yield in one step industrially advantageously, by starting from 3',4'-dideoxy-3',4'-didehydrokanamycin B via novel intermediates. n CONSTITUTION: All or part of the NH 2 groups other than the 1-position of the compound of formula I are protected by a group, e.g. tert-butoxy-carbonyl group. The resulting compound is reacted with isoserine or L-4-amino-2-hydroxy-butyric acid or their reactive derivative. The acylated product is subjected to the protecting- group removal and reduction of the 3'-and 4'-positions to give a compound of formula II (n is 1 or 2) useful as an antibacterial. The intermediate compounds of formula III (R 1 , R 2 , R 3 and R 4 are H or tert-butoxycarbonyl groups, except where all of them are H's), of formula IV (Z is benzyloxycarbonyl group), and the compound (C) after removal of protecting groups of formula IV are novel. The compound (C) is also useful as an antibacterial. n COPYRIGHT: (C)1980,JPO&Japio
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