{"id":25478,"date":"2026-05-02T18:32:16","date_gmt":"2026-05-02T22:32:16","guid":{"rendered":"https:\/\/hepatochem.com\/a-novel-cyanomethylation-method-using-the-lucent360\/"},"modified":"2026-05-02T18:32:16","modified_gmt":"2026-05-02T22:32:16","slug":"a-novel-cyanomethylation-method-using-the-lucent360","status":"publish","type":"post","link":"https:\/\/hepatochem.com\/euro\/a-novel-cyanomethylation-method-using-the-lucent360\/","title":{"rendered":"A novel cyanomethylation method using the Lucent360™"},"content":{"rendered":"

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The Lucent360™ is the most complete photochemical reactor available for controlling and screening reaction parameters;\u00a0 wavelength, light intensity, reaction time, and temperature at both small and large scale. But specs only matter when you can see how the instrument fits into a real research and development program. A recent paper from GSK shows exactly that.<\/p>\n

In Chemistry \u2014 A European Journal<\/em>, lead author Gemma Cook and coworkers report how the Lucent360™ helped them discover a new reaction and remove a highly toxic cyanide reagent from their synthesis. The paper is open access: “Expedient Discovery of a Metallaphotoredox Cyanomethylation for Synthesizing \u03b1-Aryl Nitriles.”<\/a><\/p>\n

Why \u03b1-aryl nitriles matter \u2014 and why they’re hard to make<\/h4>\n

Several marketed drugs, including Verapamil, Ariflo, and Anastrozole, contain the \u03b1-aryl nitrile motif. The nitrile group is small enough to fit tight binding pockets while still forming productive interactions with a target \u2014 and once installed, it serves as a synthetic handle for accessing amines, carboxylic acids, tetrazoles, and more.<\/p>\n

The catch: most existing methods to install this group rely on highly toxic cyanide reagents that are difficult to use at industrial scale, or require harsh conditions that limit functional group tolerance. A milder route would unlock library-scale SAR work on \u03b1-aryl nitriles.<\/p>\n

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A serendipitous discovery<\/h4>\n

While attempting a different photochemical alkylation under standard Ir\/Ni conditions, the GSK team observed an unexpected product: cyanomethylation, with the acetonitrile solvent itself coupling the aryl bromide. That observation became the starting point for a brand-new method.<\/p>\n

What followed was an extensive HTE and Design-of-Experiments campaign \u2014 optimizing photocatalyst, nickel source, ligand, base, and stoichiometries \u2014 that lowered iridium and nickel loadings without sacrificing yield.<\/p>\n

\"Lucent_experiment\"<\/p>\n

The Lucent360™ setup<\/h4>\n

The optimized conditions were applied to a substrate scope of medicinally relevant aryl bromides using the Lucent360™ in screening mode:<\/p>\n