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    Home > Active Ingredient News > Active Ingredient Products News > The Production Process of Alendronic acid

    The Production Process of Alendronic acid

    • Last Update: 2023-05-09
    • Source: Internet
    • Author: User
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    Alendronic acid is a bisphosphonate drug that is commonly used to treat osteoporosis and other conditions that affect bone health.
    The production process of alendronic acid involves several steps, which are outlined below.


    1. Synthesis of the starting material
      The first step in the production of alendronic acid is the synthesis of the starting material, which is an alkylating agent known as 1,2-bis(2,4-dichlorobenzoyl)benzene.
      This compound is synthesized by reacting 1,2-benzylene dichloride with chlorooxybenzene in the presence of a base such as sodium hydroxide.
      The resulting product is then treated with hydrazine hydrate to form the bis(2,4-dichlorobenzyl)amine, which is the desired starting material.
    2. Condensation reaction
      The next step in the production of alendronic acid is a condensation reaction, in which the starting material is treated with an acylating agent such as chloroformic acid.
      This reaction produces a compound known as 1,2-bis(2,4-dichlorobenzoyl)glycolic acid.
    3. Esterification reaction
      The 1,2-bis(2,4-dichlorobenzoyl)glycolic acid produced in the previous step is then treated with an alcohol such as methanol in the presence of a strong acid catalyst such as hydrochloric acid.
      This reaction converts the acid into an ester, known as 1,2-bis(2,4-dichlorobenzoyl)ethyl glycolate.
    4. Dehydration reaction
      The ester produced in the previous step is then treated with a dehydrating agent such as sodium hydride in the presence of a solvent such as DMF.
      This reaction removes water from the ester to form an olefin, known as 1,2-bis(2,4-dichlorobenzoyl)ethylene.
    5. Reduction reaction
      The olefin produced in the previous step is then treated with a reducing agent such as lithium aluminum hydride (LiAlH4) in the presence of an solvent such as N,N-dimethylformamide (DMF).
      This reaction reduces the double bond in the olefin to form a single bond, producing a compound known as 1,2-bis(2,4-dichlorobenzoyl)ethylamine.
    6. Nucleophilic substitution reaction
      The compound produced in the previous step is then treated with an aqueous solution of hydrogen chloride.
      This reaction, known as nucleophilic substitution, replaces the amine group in the compound with chloride ions, producing a compound known as 1,2-bis(2,4-dichlorobenzoyl)benzene.
    7. Purification and isolation
      The final step in the production of alendronic acid is the purification and isolation of the product.
      This is typically done by crystallization, which involves dissolving the crude product in a solvent and allowing it to crystallize out of solution.
      The crystals are then collected and dried to remove any remaining impurities.

    In conclusion, the production process of alendronic acid involves several steps, including the synthesis of the starting material, a condensation reaction, an esterification reaction, a dehydration reaction, a reduction reaction, and a nucleophilic substitution reaction.
    The final product is then purified and isolated through crystallization.
    This process is used to produce the active ingredient of alendronic acid for medical use.


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