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    Home > Active Ingredient News > Drugs Articles > The Upstream and Downstream products of 4-Fluoro-2-methyl-1-(1-methylethyl)-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-benzimidazole

    The Upstream and Downstream products of 4-Fluoro-2-methyl-1-(1-methylethyl)-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-benzimidazole

    • Last Update: 2023-05-13
    • Source: Internet
    • Author: User
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    4-Fluoro-2-methyl-1-(1-methylethyl)-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-benzimidazole (also known as Compound X) is a unique and complex organic compound that is used as an intermediate in the production of several pharmaceuticals and agrochemicals.
    The compound is manufactured through a series of chemical reactions that involve various upstream and downstream products.


    Upstream Products
    The production of 4-Fluoro-2-methyl-1-(1-methylethyl)-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-benzimidazole begins with the synthesis of several upstream products, including 4-fluoro-2-methyl-1H-benzimidazole, 1,1-dimethylethyl chloride, and tetrakis(rimethylhydroxymethyl)borate.
    The first step in the synthesis of these upstream products involves the reaction of 4-fluoro-2-methyl-1H-benzimidazole with 1,1-dimethylethyl chloride in the presence of a Lewis acid catalyst, such as aluminum chloride.
    This reaction forms the Grignard reagent, which is then treated with tetrakis(rimethylhydroxymethyl)borate to form the desired boronate ester.


    Downstream Products
    The boronate ester formed from the reaction of the Grignard reagent and tetrakis(rimethylhydroxymethyl)borate is then treated with aqueous sodium hydroxide solution to hydrolyze the ester and form an alcohol.
    This alcohol is then reduced using hydrogenation over a palladium catalyst to form the desired compound, 4-fluoro-2-methyl-1-(1-methylethyl)-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-benzimidazole.


    The downstream products of the synthesis of 4-fluoro-2-methyl-1-(1-methylethyl)-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-benzimidazole include several pharmaceuticals and agrochemicals, as well as other organic compounds that are used as intermediates in the production of these products.
    Some of the downstream products include the following:


    1. Pharmaceuticals:
    • Bicalutamide, which is used to treat prostate cancer
    • Fluconazole, which is an antifungal drug
    • Vinblastine, which is used to treat cancer
    • Vincristine, which is used to treat cancer
    1. Agrochemicals:
    • Isoxaben, which is a herbicide
    • Pirimicarb, which is a insecticide and acaricide

    Manufacturing Process
    The production of 4-Fluoro-2-methyl-1-(1-methylethyl)-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-benzimidazole involves several steps, including the synthesis of upstream products, the reaction of these products to form the boronate ester, the hydrolysis of the ester to form the alcohol, and the reduction of the alcohol to form the final product.


    The synthesis of the upstream products typically involves the use of various chemical reactions, such as the Grignard reaction and the hydroboration reaction.
    The reaction of these products to form the boronate ester is typically carried out in the presence of a Lewis acid catalyst, such as aluminum chloride or iron(III) chloride.
    The hydrolysis of


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