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    Home > Active Ingredient News > Antitumor Therapy > The Production Process of Fulvestrant

    The Production Process of Fulvestrant

    • Last Update: 2023-05-12
    • Source: Internet
    • Author: User
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    Fulvestrant is a synthetic steroid hormone used in cancer treatment that is produced through a complex process in the chemical industry.
    The production process of fulvestrant involves several steps, each of which requires careful attention to detail to ensure the final product is of the highest quality.


    1. Synthesis of the starting material
      The first step in the production of fulvestrant is the synthesis of the starting material, which is a compound called 7-dehydroxyprogesterone.
      This compound is synthesized through a series of chemical reactions that involve the transformation of a starting material called pregn-4-ene-3,20-dione.
    2. Cyclization reaction
      The next step in the production of fulvestrant is the cyclization reaction, where the 7-dehydroxyprogesterone molecule is converted into a cyclic compound called 1,2,6,7,8,9-hexahydro-10H-pyrano[2,3-d]pyrimidin-7-one.
      This reaction is carried out in the presence of an organic solvent and a strong acid catalyst.
    3. Amination reaction
      The next step in the production of fulvestrant is the amination reaction, where the cyclic compound from step two undergoes a reaction with an amine, typically glycine.
      This reaction is carried out in the presence of an organic solvent, and the resulting compound is called N-glycyl-1,2,6,7,8,9-hexahydro-10H-pyrano[2,3-d]pyrimidin-7-one.
    4. Esterification reaction
      The next step in the production of fulvestrant is the esterification reaction, where the N-glycyl-1,2,6,7,8,9-hexahydro-10H-pyrano[2,3-d]pyrimidin-7-one molecule is converted into an ester called N-acyl-1,2,6,7,8,9-hexahydro-10H-pyrano[2,3-d]pyrimidin-7-one.
      This reaction is carried out in the presence of a strong acid catalyst and an organic solvent.
    5. Deprotection reaction
      The final step in the production of fulvestrant is the deprotection reaction, where the N-acyl-1,2,6,7,8,9-hexahydro-10H-pyrano[2,3-d]pyrimidin-7-one molecule is converted into the final product, fulvestrant.
      This reaction is carried out in the presence of a reducing agent, such as lithium aluminum hydride, which cleaves the ester group and results in the formation of the final product.

    Overall, the production process of fulvestrant involves several complex chemical reactions that require careful attention to detail and a deep understanding of the underlying chemistry.
    Each step in the process must be carried out with precision to ensure the final product is of the highest quality and meets all the necessary specifications.


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