Stereospecific Amination of Mesylated Cyclobutanol in Continuous Flow

    • Matthieu Tissot
    • Jérôme Jacq
    • Patrick Pasau
    • UCB Biopharma SPRL, Avenue de l’industrie, 1420 Braine l’Alleud, Belgium

    We report an amination of mesylated cyclobutanol enabled by a multistep continuous flow process. The flow sequence involved an azidation followed by a Staudinger reduction which avoids the handling and isolation of a hazardous alkyl azide compound. The process is stereospecific with the azidation step proceeding to complete stereochemical inversion.

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