β, β-DISUBSTITUTED DERIVATIVES OF 9-DEOXO-9A-N-ETHENYL-9A-AZA-9A- HOMOERYTHROMYCIN A Russian patent published in 2003 - IPC

FIELD: antibiotics, chemical technology. SUBSTANCE: invention relates to β, β-disubstituted derivatives of 9-deoxo-9a-N-ethenyl-9a-aza-9a-homo- erythromycin A of the general formula (I) where R¹ and R² are similar mutually or different and mean nitrile, carboxy-group of the formula COOR³ where R³ represents C₁-C₄-alkyl group or keto- group of the formula COR⁴ where R⁴ represents C₁-C_4/ -alkyl group, and their pharmaceutically acceptable additive salts with inorganic or organic acids. Invention proposes also method of synthesis of these derivatives by carrying out reaction of 9-deoxo-9a-aza-9a-homoerythromycin A of the formula (II) with ethoxymethylene-derivatives of the general formula (III) in toluene, xylene or some other aprotonic solvents at temperature 20-115 C followed by, if necessary, with inorganic or organic acids. Compounds elicit antibacterial properties. EFFECT: improved method of synthesis, valuable medicinal properties. 14 cl