New synthesis promises to cut cost of making amine drugs

New synthesis promises to cut cost of making amine drugs

Amines are widely-used chemical intermediates and turn up in polymers, pharmaceuticals and fine chemical products, along with many pharmaceuticals and household products.Amines that contain a ring-like structure known as an aryl group are seen in pharmaceuticals such as the antipsychotic aripiprazole, cholesterol-lowerer rosuvastatin, anticancer drug imatinib and local anaesthetic lidocaine, and are also used as solvents and catalysts in drug production.Chi Wai Cheung and Xile Hu of the Ecole Polytechnique Fédérale de Lausanne have developed a new synthetic route for amines that cuts a step out of the currently-used process and makes use of less costly starting materials.While aryl amines are typically synthesised from anilines – which are in turn synthesized by hydrogenation of nitroarenes – the EPFL researchers have now developed a way to make them directly from nitroarenes, which are often cheaper than anilines, as well as alkyl halides. Using a simple iron catalyst, the researchers were able to couple amines to a number of alkyl halides, a group of organic compounds widely used in commercial products and of great usefulness in medicinal chemistry. The research is published in the journal Nature Communications.The method was shown to have a high tolerance for the addition of functional groups to the amine molecule – including groups that require protection under conventional amine synthesis – making them versatile and well suited for a broad range of applications, according to the r…

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