875573-66-3Relevant articles and documents
Impurity control method of fulvestrant
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, (2020/09/23)
The invention belongs to the field of pharmaceutical chemicals, and relates to a fulvestrant impurity control method, which is characterized in that from the introduction of chiral carbon to the synthesis of a fulvestrant intermediate compound represented by a formula VII-1, multi-step and step-by-step control is performed on 7beta isomer impurities, so that the 7beta isomer content of the VII-1 compound is between 0.1% and 0.3%, and finally the qualified fulvestrant bulk drug with stable quality is prepared. The impurity control method is simple to operate, low in production cost and high intotal yield, and can be applied to large-scale industrial production.
An alternative synthesis of the breast cancer drug fulvestrant (Faslodex): catalyst control over C-C bond formation
Caprioglio, Diego,Fletcher, Stephen P.
, p. 14866 - 14868 (2015/10/06)
Fulvestrant (Faslodex) was synthesized in four steps (35% overall yield) from 6-dehydronandrolone acetate. Catalyst controlled, room temperature, diastereoselective 1,6-addition of the zirconocene derived from commercially available 9-bromonon-1-ene was used in the key C-C bond forming step.