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ESTER DERIVE DE 7-.ALPHA.-(4,4,5,5,5-PENTAFLUOROPENTYLSULPHINYL)NONYL]OESTRA-1,3,5(10)-TRIENE-3,17BETA-DIOL AYANT UNE ACTIVITE ANTITUMORALE ET METHODE DE PREPARATION ASSOCIEE
专利权人:
LTD.;XIAN LIBANG PHARMACEUTICAL TECHNOLOGY CO.;XI'AN LIBANG PHARMACEUTICAL TECHNOLOGY CO.
发明人:
JIAO, YAQI,WANG, JIUCHENG,HU, RENLE
申请号:
CA2909418
公开号:
CA2909418A1
申请日:
2013.04.18
申请国别(地区):
CA
年份:
2014
代理人:
摘要:
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.
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