Le Quesne P W, Allam K, Abdel-Baky S, Onan K D, Purdy R H
Department of Chemistry, Northeastern University, Boston, MA 02115.
Steroids. 1989 Jun;53(6):649-61. doi: 10.1016/0039-128x(89)90058-5.
A new, short synthetic route to 2-fluoroestradiol from 19-nortestosterone is described which gives the target compound in an approximately 25% overall yield. Oxidative defluorination of 2-fluoroestradiol to 2-hydroxyestradiol via treatment with Frémy's salt/iodide ion is reported. This process is regarded as biomimetic with respect to cytochrome P-450-dependent oxidative defluorination.
描述了一种从19-去甲睾酮合成2-氟雌二醇的新的短合成路线,该路线使目标化合物的总产率约为25%。报道了通过用弗雷米盐/碘离子处理将2-氟雌二醇氧化脱氟为2-羟基雌二醇的过程。就细胞色素P-450依赖性氧化脱氟而言,该过程被认为是仿生的。