METHODOLOGY FOR THE SYNTHESIS AND SPECIFIC ACTIVITY DETERMINATION OF 16-ALPHA-[BR-77]-BROMOESTRADIOL-17-BETA AND 16-ALPHA-[BR-77]-11-BETA-METHOXYESTRADIOL-17-BETA, 2 ESTROGEN RECEPTOR-BINDING RADIOPHARMACEUTICALS
METHODOLOGY FOR THE SYNTHESIS AND SPECIFIC ACTIVITY DETERMINATION OF 16-ALPHA-[BR-77]-BROMOESTRADIOL-17-BETA AND 16-ALPHA-[BR-77]-11-BETA-METHOXYESTRADIOL-17-BETA, 2 ESTROGEN RECEPTOR-BINDING RADIOPHARMACEUTICALS
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DOI：
10.1016/0020-708x(82)90010-2
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发表时间：
1982-01-01
期刊：
影响因子：
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通讯作者：
WELCH, MJ
中科院分区：
文献类型：
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作者：
SENDEROFF, SG;MCELVANY, KD;WELCH, MJ
16.α.-[77Br]-溴雌二醇-17.β。由雌酮烯醇二乙酸酯通过用Na 77Br 和过氧化氢-乙酸溴化，然后用氢化铝锂还原得到16.α.[77Br]-溴雌二醇-17.β的混合物来合成。和16.α.-[77Br]-溴雌二醇-17.α。通过 HPLC [高压液相色谱法]，前者可以以 50% 的总放射化学收率（从 Na 77Br 中）获得。类似的程序可用于制备16α-[77Br]-溴-11.β-甲氧基雌二醇-17.β。通过与羔羊子宫雌激素受体结合测定，这些放射性药物的有效比活性为900-1500Ci/mmol。两者对雌激素受体都具有高亲和力和良好的结合选择性，可用作乳腺肿瘤的显像剂。
16.alpha.-[77Br]-Bromoestradiol-17.beta. was synthesized from estrone enol diacetate by bromination with Na 77Br and hydrogen peroxide-acetic acid, followed by reduction with lithium aluminum hydride to give a mixture of 16.alpha.[77Br]-bromoestradiol-17.beta. and 16.alpha.-[77Br]-bromoestradiol-17.alpha. from which the former can be obtained in 50% overall radiochemical yield (from Na 77Br) by HPLC [high-pressure liquid chromatography]. Analogous procedures can be used in the preparation of 16.alpha.-[77Br]-bromo-11.beta.-methoxyestradiol-17.beta.. The effective specific activities of these radiopharmaceuticals, determined by binding to the lamb uterine estrogen receptor, are 900-1500 Ci/mmol. Both have high affinity and good binding selectivity for the estrogen receptor and are useful as imaging agents for mammary tumors.