~3H-联苯双酯的合成及其稳定性的研究
STUDIES ON THE SYNTHESIS AND STABILITY OF ~3H-BIPHENYL DIESTER
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摘要: <正> 联苯双酯的化学结构为4,4′-二甲氧基-5,6,5′,6,-二次甲二氧基-2,2′-二甲氧羰基联苯,它是由中国医学科学院药物研究所合成的五味子丙素简化类似物,用于治疗慢性肝炎。为了进一步研究其吸收分布、代谢、排泄及其作用机制,尤其是利用放射免疫法测定病人血中药物浓度,以便进一步指导临床合理用药,为此我们制备了两种比活度的氚标记化合物。利用放电曝射标记法,制备的~3H-联苯双酯,比活度为7.29GBq/mmol(197Abstract: In order to investigate the absorption, distribution, metabolism and excretionmechanism of the biphenyl diester and to determine its concentration in patient'sblood for rational clinic dose dimethyl-3, 3'-dibromo-4, 4'-dimethoxy-5, 6, 5'6'-bismethylene-dioxy-2,2'-dicarboxylate was synthesized. ~3H-biphenyl diester ofhigh specific radioactivity was prepared by highvoltage-discharge catalytictritium-bromine exchange method and purified with TLC. Specific activity is 182.4GBq/mmol (4.93 Ci/mmol). Its stability was tested.