2025-09-17 産業技術総合研究所
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- https://www.aist.go.jp/aist_j/press_release/pr2025/pr20250917/pr20250917.html
- https://pubs.acs.org/doi/10.1021/acssuschemeng.5c07441
フロー反応・インライン抽出・結晶化を用いたメシル酸サフィナミドの連続合成 Continuous Synthesis of Safinamide Mesylate using Flow Reactions, Inline Extraction, and Crystallization
Kwihwan Kobayashi,Takenori Kimura,Takuya Tsubaki,Shingo Komatsuzaki,and Akira Yada
ACS Sustainable Chemistry & Engineering Published: September 3, 2025
DOI:https://doi.org/10.1021/acssuschemeng.5c07441
Abstract
Safinamide mesylate is a pharmaceutical agent approved in various countries for the treatment of Parkinson’s disease. However, owing to the lack of an efficient flow-compatible synthetic route and the requirement for intermediate purification, a continuous flow method for its synthesis has not yet been reported. In this study, we aimed to develop a fully continuous flow process to synthesize safinamide mesylate. A sequence of flow reactions, inline extraction, and crystallization steps was employed for the continuous flow synthesis of safinamide mesylate. In particular, C–O bond formation was achieved using a plug flow reactor, while reductive amination was performed in a packed-bed flow reactor. Moreover, crystallization was conducted via neutralization with methanesulfonic acid. Safinamide mesylate was obtained in an overall yield of 83% without the isolation or purification of the intermediates. The scale-up of the continuous synthesis process was successfully demonstrated, resulting in a yield and production rate of 97% and 22.0 g h–1, respectively. Our proposed method for continuous synthesis and purification could contribute to the production of various fine chemicals and pharmaceuticals.
