WATER SOLUBLE COPOLYMERS OF N-VINYL-2-PYRROLIDONE AND CROTONIC ACID DERIVATIVES HAVING GLUCOCORTICOID ACTIVITY AND PROCESS FOR PREPARATION SAID COPOLYMERS

摘要

FIELD: chemistry of high-molecular weight compounds, in particular, medicine and bioorganic chemistry, and more specifically, water soluble copolymers. SUBSTANCE: invention describes water soluble copolymers of general formula , where R₁ is H or -CH₂CH₂N(C₂H₅)₂;; R₂ is corticosteroid residue adjoined to 21-CH₂OH- group consisting of hydrocortisone and dexametasone where n is 56.4-89.8 mole%, m is 2.0-29.8 mole%, l is 5.5-13.8 mole% with molecular weight of (4-40)•10³.. Molecular weight makes it possible to provide medicinal preparations. Copolymers are prepared by copolymerization in organic solvent in inert gas consisting of N-vinyl-2-pyrrilidone, cotricosteroid and crotonic acid 21-cronotate or N, N-diethyl aminoethyl crotonate in the presence of radical initiator. Ratio of comonomers, mole%: 17.9-91.9:4.7-19.0:2.4-64.0, respectively. Total concentration of comonomers is 6-55 wt.-%. Solvent is ethanol, 2-propanol, benzene, N,N-dimethyl formamide. Resulting copolymers have improved stability to hydrolysis: under sealing conditions hydrolysis of steroid group does not occur during one-year-storage; derivative prepared by known method cleaves 28-30% of steroid for 6 months under the same conditions. EFFECT: improved properties. 5 cl, 2 dwg