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    Home > Active Ingredient News > Drugs Articles > The Synthetic Routes of Carbamimidothioic acid, [2-[(aminoiminomethyl)amino]-4-thiazolyl]methyl ester, dihydrochloride

    The Synthetic Routes of Carbamimidothioic acid, [2-[(aminoiminomethyl)amino]-4-thiazolyl]methyl ester, dihydrochloride

    • Last Update: 2023-04-26
    • Source: Internet
    • Author: User
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    Carbamimidothioic acid, [2-[(aminoiminomethyl)amino]-4-thiazolyl]methyl ester, dihydrochloride, also known as CB-5053, is an orally bioavailable, small molecule inhibitor of the bromodomain and extraterminal domain (BET) proteins.
    BET proteins are a family of transcriptional regulatory proteins that play a role in the regulation of gene expression and are implicated in various diseases such as cancer.


    There are several synthetic routes for the preparation of CB-5053, some of which are outlined below.


    1. Synthesis of 2-[(aminoiminomethyl)amino]-4-thiazolyl)methyl bromide: This step involves the synthesis of the amino acid derivative 2-[(aminoiminomethyl)amino]-4-thiazolyl)methyl bromide, which is a precursor to CB-5053.
      This can be achieved through a series of chemical reactions such as the reaction of 2-amino-4-thiazolemethionine with chloromethyl bromide in the presence of pyridine.
    2. Synthesis of [2-[(aminoiminomethyl)amino]-4-thiazolyl]methyl ester: This step involves the esterification of 2-[(aminoiminomethyl)amino]-4-thiazolyl)methyl bromide with methanol in the presence of a strong acid catalyst such as hydrochloric acid.
    3. Synthesis of CB-5053: This step involves the final step of the synthesis of CB-5053, which involves the hydrolysis of the ester obtained in step 2 to form the dihydrochloride salt.
      This can be achieved through the treatment of the ester with a strong acid such as hydrochloric acid.

    In summary, the synthesis of CB-5053 involves a series of chemical reactions that can be carried out in a variety of ways.
    The exact method used to synthesize CB-5053 will depend on the specific requirements of the synthesis and the availability of the necessary reagents and equipment.


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