3-胺基雌激素是潜在的雌激素药物,传统的合成方法以雌酚酮为原料,难以进行多样性导向的快速合成.以19-羟基雄甾-4-烯-3,7-二酮为原料,利用串联的retro-aldol芳构化/分子内亲核加成高效合成了6-取代-3-胺基雌激素.该方法试剂易得,操作简单,可一步反应同时导入两个取代基. 3-Amino estrogen is a potential estrogen drug, and the traditional synthesis method uses estrone as a raw material, so that it is difficult to conduct rapid diversification-oriented synthesis.Using 19-hydroxyandrost-4-ene-3,7-dione As the starting material, 6-substituted-3-amino estrogens were efficiently synthesized by a series of retro-aldol aromatization / intramolecular nucleophilic addition.The reagents of this method were easy to obtain, easy to operate and could be introduced into two substitutions base.