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。
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.
出处
《复旦学报（医学版）》
EI
CAS
CSCD
北大核心
2003年第5期494-495,共2页
Fudan University Journal of Medical Sciences
