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    Home > Active Ingredient News > Antitumor Therapy > The Synthetic Routes of Lapatinib

    The Synthetic Routes of Lapatinib

    • Last Update: 2023-04-26
    • Source: Internet
    • Author: User
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    Lapatinib is a synthetic drug that is used to treat various types of cancer, including breast cancer and ovarian cancer.
    It is a targeted therapy drug that works by inhibiting the HER2 receptor tyrosine kinase, which is involved in cell growth and division.
    The development of lapatinib is a complex process that involves several synthetic routes.


    The first synthetic route of lapatinib involves a multi-step process that starts with the synthesis of the natural product, yew poison.
    Yew poison is a plant-derived alkaloid that contains a lactone moiety, which is the core structure of lapatinib.
    The synthesis of yew poison involves the isolation of the precursor alkaloid from the yew plant, followed by a series of chemical reactions to convert it into the desired lactone moiety.


    The next step in the synthesis of lapatinib involves the introduction of the bis(2-oxo-3-oxazolidinyl) phosphate (BOOP) moiety into the lactone precursor.
    This involves a condensation reaction between the lactone and an amino acid, followed by a series of chemical transformations to introduce the BOOP moiety.


    The final step in the synthesis of lapatinib involves the attachment of a purine-based sidechain to the BOOP moiety.
    This involves a series of condensation and reduction reactions to form the desired sidechain.


    Another synthetic route of lapatinib involves a two-step process that starts with the synthesis of the natural product, camptothecin.
    Camptothecin is a plant-derived alkaloid that contains a lactone moiety, which is similar to the lactone moiety in lapatinib.
    The synthesis of camptothecin involves the isolation of the precursor alkaloid from the camptothecin plant, followed by a series of chemical reactions to convert it into the desired lactone moiety.


    The next step in the synthesis of lapatinib involves the introduction of the BOOP moiety into the camptothecin lactone precursor.
    This is similar to the first synthetic route, and involves a condensation reaction between the lactone and an amino acid, followed by a series of chemical transformations to introduce the BOOP moiety.


    The final step in the synthesis of lapatinib using this route involves the attachment of a purine-based sidechain to the BOOP moiety.
    This is also similar to the first synthetic route, and involves a series of condensation and reduction reactions to form the desired sidechain.


    Overall, the synthetic routes of lapatinib involve a combination of organic synthesis and chemical transformations, and require a high degree of skill and expertise.
    The development of these synthetic routes has enabled the large-scale production of lapatinib for use in cancer treatment.
    However, these routes are complex and expensive, and there is ongoing research to develop more efficient and cost-effective synthetic routes for this important drug.


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