FIELD: organic chemistry, chemical technology, antibiotics.
SUBSTANCE: derivative of 9-deoxo-9a-aza-9a-homoerythromycin A of the formula (3) wherein R4 represents hydroxyl protecting group is prepared by protection of 2'-hydroxy-group of compound of the formula (5) to form compound of the formula (4) 
and by oxidation of C-4''-hydroxy-group of compound of the formula (4) that is carried out by addition of dimethylsulfoxide to solution containing compound of the formula (4) and a solvent followed by cooling the mixture up to about -70°C, activation of dimethylsulfoxide in situ and defoaming the reaction mixture. Compound of the formula (4) is converted to the oxidation stage directly without its isolation. Also, invention proposes additive salt of trifluoroacetic acid of compound of the formula (3) and a method for its preparing by treatment of compound of the formula (3) with trifluoroacetic acid. Invention provides increasing yield and improving purity of the end product.
EFFECT: improved preparing method.
11 cl, 6 ex
| Title | Year | Author | Number |
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| DERIVATIVES OF QUINOLINE CARBOXYLIC ACID, MIXTURE OF ISOMERS OR INDIVIDUAL ISOMERS, THEIR PHARMACEUTICALLY ACCEPTABLE HYDRATES AND SALTS, METHOD FOR THEIR PRODUCTION | 1992 |
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