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

    The Synthetic Routes of Lestaurtinib

    • Last Update: 2023-04-25
    • Source: Internet
    • Author: User
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    Lestaurtinib, also known as CEP-11985 or SP32336, is a novel oral small molecule inhibitor of the Bruton's tyrosine kinase (BTK) with potential antineoplastic activity.
    It is being developed as a treatment for various types of cancer, including leukemia and lymphoma.
    In the chemical industry, the synthesis of lestaurtinib is a complex and multi-step process that involves the synthesis of several intermediate compounds.


    One of the most commonly used synthetic routes for lestaurtinib involves the following steps:


    1. Synthesis of the aminothiazole starting material: This is accomplished by a series of chemical reactions involving the reaction of an appropriate starting material with chloramine T and an amine, followed by treatment with a sulfurizing agent and reduction with hydrogen.
    2. Synthesis of the 3-bromo-1H-indolez-2-one: This compound is prepared by a Suzuki-Miyaura coupling reaction between the aminothiazole from step 1 and a brominated arylboron reagent.
    3. Synthesis of the 2-[(2S)-2-(4-chlorophenyl)-2-oxo-1,3-oxazolidin-3-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-amine: This key intermediate is prepared by a series of chemical reactions involving the condensation of the 3-bromo-1H-indolez-2-one from step 2 with a brominated arylboron reagent, followed by treatment with a chlorinating agent and a series of reduction and deprotection steps.
    4. Synthesis of the final product: This is accomplished by a series of chemical reactions involving the condensation of the intermediate from step 3 with a series of other chemicals, followed by reductive amination and deprotection steps.

    Overall, this synthetic route requires the use of several specialized reagents and methods, and can take several steps to complete.
    However, it is a commonly used route for the synthesis of lestaurtinib, and has been reported in a number of research articles and patents.


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