ESTER DERIVATIVES OF 7--9-(4,4,5,5,5-PENTAFLUOROPENTYLSULFINYL)NONYL-ESTRA-1,3,5(10)-TRIENE-3,17-DIOL HAVING ANTICANCER ACTIVITY AND PREPARATION METHOD THEREOF

摘要

The present invention provides a class of full-vantex ester derivatives and methods for their preparation. Such compounds are aliphatic esters having the structure of the formula: formed by esterifying the C-3 position of the fulvestrant and the -OH at the C-17 position: (A) In the above formula, the substituent R may be a hydrogen atom, an alkanoyl or alkenoyl of 2 to 22 carbon atoms, or a stereoisomer thereof; Substituent R 'can be a hydrogen atom, an alkanoyl or alkenoyl having 2 to 4 carbon atoms, or a stereoisomers thereof; Such an aliphatic ester compound is used as a prodrug for improving the stability of the compound, while the decrease in polarity can easily make them lipid emulsions, microspheres and the like, and the compound is decomposed by factors such as high temperature and the like Can be prevented.