DERIVATIVES OF AZITHROMYCIN AND METHOD FOR THEIR PREPARING Russian patent published in 2003 - IPC

FIELD: organic chemistry, antibiotics. SUBSTANCE: invention relates to derivatives of azithromycin of the general formula (I) wherein R¹ means hydroxyl group or L-cladinosyl group of the formula (II) wherein R² means hydrogen atom or trimethylsilyl group; R³ means hydrogen atom or in common with R⁶ it means simple ether group; R⁴ means hydrogen atom, acetyl or benzyloxycarbonyl; R⁵ means hydrogen atom, methyl or benzyloxycarbonyl; R⁶ means hydroxyl group or in common with R³ it means simple ether group; R⁷ and R⁸ mean hydrogen atom, (C₁-C₄)- alkyl group or in common with C-11/C-12 carbon atom they mean cyclic carbonate; or R⁷ means trimethylsilyl group, and to their pharmaceutically acceptable additive salts of inorganic or organic acids. Invention proposes also method for preparing these compounds. Compounds elicit antibacterial activity and can be used as intermediate compounds for preparing macrolide antibiotic of 9a-azalides class. EFFECT: improved preparing method, valuable medicinal properties. 23 cl, 2 tbl, 18 ex