FIELD: chemistry.
SUBSTANCE: invention relates to method of obtaining (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid, including: i) opening of epoxy cycle of Compound 3 by means of methylamine with obtaining compound 4, ii) separation of Compound 4 by means of chiral acid, selected from L-(-)-malic acid and L-(-)-pyroglutamic acid with obtaining Compound 5A or 5B, or iii protection of secondary amine of Compound 5A or 5B with tert-butoxycarbonyl protective group with obtaining compound 6 iv) methylation of free hydroxyl group of Compound 6 with methylating agent, v) removal of protection from amino groups by means of monohydrate of p-toluenesulphonic acid with obtaining Compound 8 and vi) interaction of Compound 8 with compound 10 with the following obtaining (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid.
EFFECT: method improvement.
29 cl, 3 tbl, 4 ex
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Author |
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METHODS OF APPLYING (+)-1,4-DIHYDRO-7-[(3S, 4S)-3-METHOXY-4-(METHYLAMINO)-1-PYRROLIDINYL]-4-OXO-1-(THIAZOLYL)-1,8-NAPHTHIRIDINE-3-CARBOXYLIC ACID FOR CANCER TREATMENT |
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