CA2909418A1 — Ester derivative of 7-.alpha.-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)n onyl]-estra-1,3,5(10)-triene-3,17.beta.-diol having anticancer activity and preparation method thereof

USPTO Abstract

The present invention provides a class of fulvestrant ester derivatives and a preparation method thereof. Such a compound is an aliphatic ester compound formed by esterifying the -OH on positions C-3 and C-17 of the fulvestrant, having a structure of the following formula. In the formula, the substituent R is H, an alkylacyl having 2-22 carbon atoms, an alkenylacyl or a stereoisomer thereof; the substituent R' can be H, an alkylacyl having 2-4 carbon atoms, an alkenylacyl or a stereoisomer thereof; such an aliphatic ester compound being used as a pro-drug can improve the stability of a compound, meanwhile the decrease of polarity can enable them to be easily made into preparations such as lipid emulsions, microspheres etc., and avoids the degradation of the compound caused by factors such as a high temperature and so on and the use of an organic solvent during the preparation process.