Stereospecific amination of mesylated cyclobutanol in continuous flow

• Matthieu Tissot^a
• Jérôme Jacq^a
• Patrick Pasau^a

• UCB Biopharma SPRL, Avenue de l’industrie, 1420 Braine l’Alleud, Belgium^a

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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