511545-93-0Relevant academic research and scientific papers
Fulvestrant: From the laboratory to commercial-scale manufacture
Brazier, Eve J.,Hogan, Philip J.,Leung, Chiu W.,O'Kearney-McMullan, Anne,Norton, Alison K.,Powell, Lyn,Robinson, Graham E.,Williams, Emyr G.
, p. 544 - 552 (2011/07/30)
The development of a commercial manufacturing process for fulvestrant (the active ingredient in 'Faslodex') is described. Key steps in the synthesis are stereoselective 1,6-addition of an organocuprate to a steroidal dienone followed by copper-mediated aromatisation of the A-ring. The strategy for dealing with noncrystalline intermediates is outlined. The production of drug substance of acceptable quality is critically dependent on limiting the formation of key impurities. The origin of these impurities is discussed, and measures to prevent or control their formation are described.
