FIELD: chemistry.
SUBSTANCE: invention describes a method of producing anthracycline of formula (1) 
from 13-daunorubicin via acylation. N-trifluoroacetyl-13-duanorubicin reacts with an aprotic solvent and an acetylation reagent to form an intermediate sulphoxy salt which is treated with a strong base to obtain 4'-keto-N-trifluoroacetyl daunorubicin. The 4'-keto-N-trifluoroacetyl daunorubicin reacts with a reducing agent such as a boron hydride of an alkali metal to obtain N-trifluoroacetyl-4'-epidaunorubicin. The N-trifluoroacetyl-4'-epidaunorubicin is hydrolysed in an alkaline solvent to obtain an intermediate compound. The intermediate compound reacts with a halogenation agent to obtain a 14-Hal-derivative. The 14-Hal-derivative is hydrolysed in the presence of a formate of an alkali metal to obtain the required end product.
EFFECT: novel method of obtaining epirubicin is described, which is characterised by high output of the end product.
17 cl, 5 ex
| Title | Year | Author | Number |
|---|---|---|---|
| METHOD OF PRODUCING 4-DEMETHYLDAUNORUBICIN | 2006 |
|
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| METHOD OF ARALKYLATION OF 4'-HYDROXYL GROUP OF ANTHRACYCLINES | 2008 |
|
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| METHOD OF OBTAINING 4-R-SUBSTITUTED 4-DEMETHOXYDAUNORUBICIN | 2004 |
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| ANTHRACYCLIN DERIVATIVES | 1995 |
|
RU2159619C2 |
| ANTHRACYCLINE DERIVATIVES, METHOD OF PRODUCING 13-BENZENIDESULPHONYLHYDRAZINE DERIVATIVES OF ANTHRACYCLINES, METHOD OF PRODUCING 13-DEOXYANTHRACYCLINES, METHOD OF PRODUCING 5-IMINO-13-DEOXYANTHRACYCLINES | 2005 |
|
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| METHOD OF OBTAINING 4-DEMETHOXYDAUNORUBICINE | 2012 |
|
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| METHOD OF PREPARING SUBSTITUTED ANTHRACYCLINE CHLOROHYDRATES | 0 |
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| METHOD OF PREPARING ANTHRACYCLINES | 0 |
|
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| METHOD OF PRODUCING 4'-DEOXY-DAUNORUBICYN OR 4'-DEOXY-DOXORUBICYN | 0 |
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| METHOD OF OBTAINING 4Ъ-HALOID-ANTHRACYCLING LICOSIDES | 0 |
|
SU1579465A3 |
