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在进行雌激素的生理、生化、代谢等研究中,迫切需要高比活的同位素标记雌二醇。9,11位标记的雌二醇可由△~(1,3,5(10),9(11))-雌甾四烯-3,17β-二醇(简称△~(9(11))-E_2)经上氘或氚而制得。对△~(9(11))-E_2的合成,文献报道较多,国内也有一些单位已进行研究。雌甾由于含有芳环A,其9α-H较活泼,故可采用各种脱氢法直接引入△~(9(11))双键。文献上有:超酸脱氢法、电解脱氢法和DDQ脱氢法等。前二法因需用特殊试剂和仪器设备而难于普遍采用,故国内多用后法。但DDQ法产物复杂,收率很低,而且由于雌二醇与△~(9(11))-E_2层析行为极为
In the study of estrogen’s physiology, biochemistry and metabolism, there is an urgent need for high specific activity of isotope labeled estradiol. The estradiol with the 9 and 11 positions could be expressed by △ ~ (1,3,5 (10), 9 (11)) - estratriene - 3,17β - diol E_2) by deuterium or tritium in the system. For the synthesis of △ ~ (9 (11)) - E_2, there are many reports in the literature and some units in China have been studied. Because estrone contains aromatic ring A, its 9α-H is more active, so various kinds of dehydrogenation can be used to introduce △ 9 (11) double bond directly. The literature includes: super acid dehydrogenation, electrolytic dehydrogenation and DDQ dehydrogenation and so on. The first two because of the need for special reagents and equipment and difficult to universally used, so the domestic use of post-law. However, the DDQ method is complicated and the yield is very low. Moreover, the chromatographic behavior of estradiol and Δ ~ (9 (11)) - E_2 is extremely