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高分子载体药物的研究:聚乙二醇-雌激素类化合物的合成
引用本文:郑虎,翁玲玲,王钢立,邓力. 高分子载体药物的研究:聚乙二醇-雌激素类化合物的合成[J]. 药学学报, 1987, 22(8): 637-640
作者姓名:郑虎  翁玲玲  王钢立  邓力
作者单位:华西医科大学药物研究所 成都(郑虎,翁玲玲,王钢立),华西医科大学药物研究所 成都(邓力)
摘    要:
聚乙二醇(PEG,I)是一种聚醚类线性高分子化合物。无论分子最多少,每一分子中都只有两个末端羟基。HO-(CH_2CH_2O-)_nCH_2CH_2OH I 1972年西德Mutter及Bayer利用其作为可溶性高分子支持剂于多肽合成,取得满意结果。之后Kster报道了它在核苷合成中的应用。近年来Bayer及Zheng等在聚乙二醇

关 键 词:聚乙二醇  雌激素  雌二醇  乙炔雌二醇
收稿时间:1986-10-28

STUDIES ON POLYMER-SUPPORT DRUG: SYNTHESIS OF PEG-ESTROGEN COMPOUNDS
ZHENG Hu,WENG Ling-Ling,WANG Gang-Li and DENG Li. STUDIES ON POLYMER-SUPPORT DRUG: SYNTHESIS OF PEG-ESTROGEN COMPOUNDS[J]. Acta pharmaceutica Sinica, 1987, 22(8): 637-640
Authors:ZHENG Hu  WENG Ling-Ling  WANG Gang-Li  DENG Li
Abstract:
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 ~(13)CNMR. 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.
Keywords:Polyethyleneglycol(PEG)  Estrogen  Estrodiol(E)  Ethinyl Estrodiol(EE)
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