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17α-乙炔雌三醇,化学名:17α-乙炔雌甾-1,3,5(10)-三烯-3,16α,17β-三醇。药理实验证明它对放疗和化疗所致的白细胞减少症显示出较好的防治效果。其作用类似雌三醇,口服效果优于雌三醇。为了深入了解该药在动物体内的作用特点和药物的代谢途径,特合成9,11位氚标记的17α-乙炔雌三醇。我们采用3,16α-双乙酰氧基雌甾-1,3,5(10)-三烯-17-酮为原料,经过DDQ[2,3-二氯,5,6-二氰苯醌]脱氢和氚化、乙炔化等反应,再以缩丙酮反应分离除去17α-异构体,得9α,11ξ-~3H-17α-乙炔雌三醇,具体合成路线如下:
17α-ethinyl estriol, chemical name: 17α-ethinyl estra-1,3,5 (10) -triene-3,16α, 17β-triol. Pharmacological experiments show that it shows good control effect on radiotherapy and chemotherapy-induced leukopenia. Its role is similar to estriol, orally better than estriol. In order to further understand the role of the drug in animals and the metabolic pathways of drugs, special synthesis of tritiated 9, 11 t-ethinyl estriol. We used 3,16α-bisacetoxyestra-1,3,5 (10) -triene-17-one as starting material and DDQ [2,3-dichloro-, 5,6-dicyanobenzoquinone] Dehydrogenation and tritiation, such as the reaction of acetylation, and then acetal reaction isolated 17α-isomer separation, 9α, 11ξ- ~ 3H-17α-ethinyl estriol, the specific synthetic route is as follows: