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    Home > Chem. Commun.: Suzuki miyaara reaction is applied to the synthesis of drugs rich in SP3 hybrid atoms

    Chem. Commun.: Suzuki miyaara reaction is applied to the synthesis of drugs rich in SP3 hybrid atoms

    • Last Update: 2017-12-27
    • Source: Internet
    • Author: User
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    An increasingly important consideration in modern pharmaceutical chemistry is the overall control of the physical and chemical properties of candidate drugs With regard to this high-level objective, the focus is on the increase in saturation (i.e fewer aromatic rings) as it relates to the possibility of improving physical properties (e.g high solubility) More SP3 hybrid atoms give the candidate drugs unique three-dimensional properties, allowing molecular screening in a wider range of chemical space In addition, higher saturation (i.e more aromatic rings or heterocycles) is believed to increase the likelihood of clinical success The general design principles discussed above are obvious in the molecules appearing in the pharmaceutical chemistry laboratory There are few aromatic rings in these compounds, which are often represented by c-aryl-linked saturated heterocycles These efforts have provided a range of compounds for drug screening and have been linked to a wide range of biological activities At present, the effective method to synthesize this new molecule is usually involved in the catalysis of organometallic reagents (boron, zinc, tin or magnesium) to form sp2-sp3 bond There are many disadvantages in the available methods, which often lead to the failure to synthesize target molecules in a high flux way About the optimization of catalyst loading and additives (source: chem Commun.) now, a research team from Strathclyde University and AstraZeneca, UK, led by Craig Jamieson, has found a new method to prepare molecules rich in SP3 hybrid atoms The strategy involves cross coupling of vinyl halide and Suzuki miyaara of vinyl borate, then reducing the newly formed olefins in one pot to produce the sp2-sp3 connection system needed So far, Craig Jamieson's team has used this method to synthesize 55 kinds of molecules rich in SP3 hybrid atoms with high yield It has also been proved that it is suitable for high-throughput parallel synthesis methods commonly used in drug screening The main advantage of this method is the practicability of one pot method and its application in a variety of synthesis targets The method can also elegantly avoid side effects And because it is a two-step one pot method, which is simple and practical, with high and consistent yield and less by-products, it is very suitable for the synthesis of a variety of analogues for drug screening At present, the main limitation of this method is that chiral raw materials are the only way to prepare chiral products In the future, the focus will be on the use of chiral catalysts for chiral synthesis, as well as larger scale synthesis applications, and the expansion of their applicability Paper link: http://pubs.rsc.org/en/content/articlelanding/2018/cc/c7cc08670a ා! Divabstract correspondent: Dr Craig Jamieson https://
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