An alternative synthesis of the breast cancer drug fulvestrant (Faslodex®): catalyst control over C-C bond formation.

Caprioglio D, Fletcher SP

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.

Keywords:

Breast Neoplasms

,

Estradiol

,

Antineoplastic Agents

,

Catalysis

,

Fulvestrant