【摘要】 目的　合成抗肿瘤新药新生血管形成抑制剂 2 甲氧基雌二醇。方法　以雌二醇为原料经 2 位溴代 ,继而甲氧基化直接合成 2 甲氧基雌二醇。结果　改进的合成方法割除了文献报道方法中的 3,17 双乙酰化及水解二个反应步骤 ,合成获得的 2 甲氧基雌二醇成品进行了结构确证。结论　通过有效地纯化 2 溴雌二醇中间体 ,可缩短二步反应直接制得成品。更多还原

【Abstract】 Purpose To synthesize a new antitumor drug 2-methoxyestradiol which is an angiogenesis inhibitor. Methods 2-methoxyestradiol was directly synthesized by 2-bromination followed methoxylation from estradiol. Results Compared with reported method,two reaction stages (3,17-diacetylation and hydrolysis) were omitted in improved synthesis.The structure of obtained 2-methoxyestradiol was confirmed via 1H?NMR and mass spectrum. Conclusions The two reaction stages in reported synthetic procedure of 2-methoxyestrdiol can be shortened via efficient purification of 2-bromoestradiol intermediate.更多还原