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以17α-炔雌二醇和17β-雌二醇为原料,分别与烯丙基溴、溴代异戊烯反应,通过一步反应合成了4个新雌激素衍生物,分别是17α-炔雌二醇-3-烯丙基醚(ES-1),17β-雌二醇-3-烯丙基醚(ES-2),17α-炔雌二醇-3-异戊烯基醚(ES-3)和17β-雌二醇-3-异戊烯基醚(ES-4),产率分别为92.2%,73.7%,65.9%和67.6%.化合物通过1HNMR,13CNMR,IR,MS及元素分析确证了结构,4个化合物均未见文献报道.初步的抗辐射升白生物活性研究表明,4个化合物对137Csγ-射线引起的小鼠白细胞低下及造血系统功能损伤有一定的保护作用.其中ES-3的升白作用最佳,经统计学处理,3个给药剂量组与对照组比,升白作用均有非常显著性差异(P<0.001).
17α-ethinyl estradiol and 17β-estradiol were used as starting materials to react with allyl bromide and bromo-isoamylene respectively. Four new estrogenic derivatives were synthesized by one-step reaction, which were 17α-ethynylestradiol Estradiol-3-allyl ether (ES-2), 17α-ethynylestradiol-3-isopentenyl ether (ES-3) And 17β-estradiol-3-isopentenyl ether (ES-4) were obtained in yields of 92.2%, 73.7%, 65.9% and 67.6%, respectively.The compounds were characterized by 1HNMR, 13CNMR, IR, MS and elemental analysis Structure and four compounds have not been reported in the literature.A preliminary study on the biological activity of anti-radiation lightening showed that the four compounds have a certain protective effect on 137Csγ-ray-induced mouse leukopenia and hematopoietic system injury.Especially ES-3 Of the best lightening effect, the statistical analysis, the three dose groups compared with the control group, the role of lightening has a very significant difference (P <0.001).