GW-250495

Chemical Name: 16alpha,17alpha-[(R)-Butylidenedioxy]-6alpha,9alpha-difluoro-11beta-hydroxy-3-oxo-4-androstene-17beta-carbothioic acid S-(2-oxotetrahydrofuran-3-y) ester
项目整合开发状态: Phase I
项目研究机构: GlaxoSmithKline (Originator)
合成路线:Treatment of carboxylic acid (I) with diethyl chlorophosphate (II) in the presence of Et3N furnished the corresponding mixed anhydride (III).This was then condensed with the sodium salt of alpha-mercapto-gamma-butyrolactone (IV) to produce the title thioester.

合成路线:The title compound was prepared by condensation of the carbothioic acid (I) with alpha-bromo-gamma-butyrolactone (II) in the presence of K2CO3 in DMF.
📌 参考资料/链接:
参考文献标题:Lactone derivs.of 17beta-carboxy,carbothio and amide androstane derivs.
文献作者:Biggadike,K.; Procopiou,P.A.(Glaxo Wellcome plc)
参考来源:JP 1999501675; US 6197761; WO 9724365