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Synthesis
DOI: 10.1055/a-2744-6831
Paper
Published as part of the Bürgenstock Special Section 2025 – Future Stars in Organic Chemistry

All-step Mechanochemical Approach for the Rapid and Solventless Synthesis of Boscalid

Autor*innen

  • Asahi Nagao

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

  • Koji Kubota

    1   Graduate School of Engineering, 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   Graduate School of Engineering, 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)

Gefördert durch: Japan Science and Technology Corporation JPMJCR19R1, JPMJFR201I
The authors gratefully acknowledge financial support from JSPS KAKENHI grants 24H00453 (to K.K.), 24H01050 (to K.K.), 24H01832 (to K.K.), 22H00318 (to H.I.), and 22K18333 (to H.I.), as well as from the JST via CREST grant JPMJCR19R1 (to H.I.) and FOREST grant JPMJFR201I (to K.K.). The authors are also grateful to the Institute for Chemical Reaction Design and Discovery (ICReDD), established by the World Premier International Research Initiative (WPI), MEXT, Japan.
Gefördert durch: Japan Society for the Promotion of Science 22H00318,22K18333,24H00453,24H01050,24H01832
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Graphical Abstract

Abstract

Boscalid, the active ingredient in various fungicides used in large quantities worldwide, is traditionally synthesized using solution-based 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 large amounts of solvent, both of which are required under conventional solution-based conditions. Furthermore, gram-scale synthesis was successfully achieved without any yield loss at each step, highlighting the potential scalability of this protocol.

Keywords

Mechanochemistry - Ball milling - Suzuki–Miyaura coupling - Boscalid - Mechanochemical synthesis

Supplementary Material



Publikationsverlauf

Eingereicht: 23. September 2025

Angenommen nach Revision: 11. November 2025

Accepted Manuscript online:
11. November 2025

Artikel online veröffentlicht:
02. Januar 2026

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