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Synthesis
DOI: 10.1055/a-2744-6831
Paper

All-step mechanochemical approach for the rapid and solventless synthesis of Boscalid

Authors

  • Asahi Nagao

    1   Division of Applied Chemistry, Hokkaido University, Sapporo, Japan (Ringgold ID: RIN12810)

  • Koji Kubota

    1   Division of Applied Chemistry, Hokkaido University, Sapporo, Japan (Ringgold ID: RIN12810)
    2   Institute of Chemical Reaction Design and Discovery (WPI-ICReDD), Hokkaido University, Sapporo, Japan (Ringgold ID: RIN12810)

  • Hajime Ito 

    1   Division of Applied Chemistry, Hokkaido University, Sapporo, Japan (Ringgold ID: RIN12810)
    3   Institute for Chemical Reaction Design and Discovery (WPI-ICReDD), Hokkaido University, Sapporo, Japan (Ringgold ID: RIN12810)

Supported by: Japan Science and Technology Corporation JPMJCR19R1, JPMJFR201I
Supported by: Japan Society for the Promotion of Science 22H00318,22K18333,24H00453,24H01050,24H01832
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Boscalid, the active ingredient in various fungicides used in large quantities worldwide, is traditionally synthesized using solutionbased methods that require substantial quantities of reaction solvents and prolonged reaction times, highlighting opportunities for improvement in waste reduction, time efficiency, and energy consumption. Herein, we report a solventless and rapid synthesis of Boscalid via an all-step mechanochemical reaction. This synthetic route comprises three steps: Suzuki-Miyaura cross-coupling, zinc-mediated Béchamp reduction, and amidation with 2-chloronicotinyl chloride. Each mechanochemical reaction proceeded rapidly, and the total reaction time was significantly shorter than that of previous methods. Notably, all synthetic operations can be carried out without an inert gas atmosphere or a large amount of solvent, both of which are required under conventional solution-based conditions. Furthermore, gramscale synthesis was successfully achieved without any yield loss at each step, highlighting the potential scalability of this protocol.



Publication History

Received: 23 September 2025

Accepted after revision: 11 November 2025

Accepted Manuscript online:
11 November 2025

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