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    Home > Chemicals Industry > Chemical Technology > Issue 4, 2022 - New method developed for synthesizing NSAIDs precursors

    Issue 4, 2022 - New method developed for synthesizing NSAIDs precursors

    • Last Update: 2022-11-14
    • Source: Internet
    • Author: User
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    Recently, Professor Mao Jianyou's research group of Nanjing University of Technology has developed a method for co-catalyzing photocatalysts
    and transition metal catalysts.
    This method uses cheap and readily available olefins, aryl halides and alkyl halides as reaction starting materials to synthesize a series of chiral α-aryl propionate compounds
    .
    This kind of compound can be used as a precursor of non-steroidal anti-inflammatory drugs and has a wide range of application value
    .

    Using dihydropyridine as a reducing agent and using the strategy of photocatalyst and nickel catalyst to synergize catalysis, the research group developed a three-component asymmetric reduction cross-coupling reaction with mild conditions, wide application range of raw materials and excellent enantioselectivity to efficiently synthesize a series of chiral α-aryl propionate compounds
    .
    Further hydrolysis of this ester compound yields a series of α-arylpropionic acid compounds
    .

    Chiral α-arylpropionic acid compounds are an important branch of the large family of anti-inflammatory drugs, and naproxen, ibuprofen, flurbiprofen, etc.
    belong to this branch
    .
    These compounds do not contain steroidal structures, so they are also called non-steroidal anti-inflammatory drugs, which have the characteristics of strong efficacy, low side effects and low toxicity, and are one of
    the most used drug types in the world.
    With the discovery and application of asymmetric catalytic synthesis, the preparation of α-arylpropionic acid compounds has become more efficient, convenient and green and economical, which has greatly promoted the development of
    non-steroidal anti-inflammatory drugs.

    Mao Jianyou said that although there are many traditional synthesis methods of α-arylpropionic acid compounds, some of these methods are cumbersome, labor-intensive and costly, and some are less suitable raw materials and the reaction is not safe
    enough.
    Qian Pengcheng, a member of the research group, said that the raw materials used in the method are simple and easy to obtain, easy to operate, and the photocatalyst and the alkali used in the reaction can be recycled and reused
    .
    These advantages highlight the value of the results in drug synthesis and modification and industrial application value
    .
    At present, the research group is also studying the synthesis of more valuable molecular structures
    .



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