Two-step continuous flow-driven synthesis of 1,1-cyclopropane aminoketones

Velichko, Viktoria;Moi, Davide;Soddu, Francesco;Scipione, Roberto;Podda, Enrico;Luridiana, Alberto;Cambie, Dario

;Secci, Francesco

;Cabua, Maria Chiara

2024-01-01

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Abstract

The continuous flow telescoped synthesis of 1,1-cyclopropane aminoketones was achieved by optimizing the photocyclization of 1,2-diketones to 2-hydroxycylobutanones (HCBs) and their reaction with aryl- and alkylamines, via tandem condensation C4-C3-ring contraction reaction. With the achieved operational conditions, we were able to obtain a library of cyclopropylamines with good chemical yields, high productivity, and short residence times.