STUDIES ON POLYMER-SUPPORT DRUG: SYNTHESIS OF PEG-ESTROGEN COMPOUNDS

Estrogen denotes a kind of steroidal hormone and has strong physiological activity. PEG is a polymer with good solubility both in water and in organic solvents. We hope to change the solubility and drug metabolism kinetic behavior of estrogen by connecting PEG to estrogen in order to apply polymer in medical chemistry. In the present paper, four new PEG-estrogen compounds were prepared and their structures determined by UV, IR, and ¹³CNMR. Estrodiol(E) and Ethinyl Estrodiol(EE)were selected as low-molecular weight drugs. The procedure for synthesis reported in this paper: first the terminal hydroxyl groups in PEG were substituted by chlorine-atom; then the chlorinated PEG reacted with E-3-Na and EE-3-Na to form the title compounds. Initial pharmacological tests indicated that the new compounds retain the some estrogenic action.