Lista Liliana, Manini Paola, Napolitano Alessandra, Pezzella Alessandro, d'Ischia Marco
Department of Organic Chemistry and Biochemistry, University of Naples Federico II, Italy.
Steroids. 2006 Aug;71(8):670-3. doi: 10.1016/j.steroids.2006.04.002. Epub 2006 May 30.
An efficient one-pot procedure for the preparation of 10beta,17beta-dihydroxyestra-1,4-dien-3-one (p-quinol, 1, 75%) is reported, involving oxidation of 17beta-estradiol with potassium permanganate. Similar treatment of 17beta-estradiol with sodium chlorite led to 10beta-chloro-17beta-hydroxyestra-1,4-dien-3-one (2) in 44% yield along with smaller amounts 4-chloro-10beta,17beta-dihydroxyestra-1,4-dien-3-one (3), 2,10beta-dichloro-17beta-hydroxyestra-1,4-dien-3-one (4), and 4,10beta-dichloro-17beta-hydroxyestra-1,4-dien-3-one (5).
报道了一种高效的一锅法制备10β,17β - 二羟基雌甾 - 1,4 - 二烯 - 3 - 酮（对苯二酚，1，产率75%）的方法，该方法涉及用高锰酸钾氧化17β - 雌二醇。用亚氯酸钠对17β - 雌二醇进行类似处理，得到10β - 氯 - 17β - 羟基雌甾 - 1,4 - 二烯 - 3 - 酮（2），产率为44%，同时还生成少量的4 - 氯 - 10β,17β - 二羟基雌甾 - 1,4 - 二烯 - 3 - 酮（3）、2,10β - 二氯 - 17β - 羟基雌甾 - 1,4 - 二烯 - 3 - 酮（4）和4,10β - 二氯 - 17β - 羟基雌甾 - 1,4 - 二烯 - 3 - 酮（5）。
