First Example of a Continuous-Flow Carbonylation Reaction Using Aryl Formates as CO Precursors

The first continuous flow carbonylation reaction using aryl formates as CO precursor is reported. The reaction is practical, scalable and high yielding. The use of a flow protocol safely allows expanding the scope to activated chlorides, nitrogen heterocycles and to the selective introduction of an ester group in dihalo-derivatives. Further selective reduction of the ester formed to an aldehyde in flow is also described.

• Nerea Alonso^1,3
• Juan de Muñoz¹
• Brecht Egle²
• Johannes L. Vrijdag²
• Wim M. De Borggraeve²
• Antonio de la Hoz³
• Angel Díaz-Ortiz³
• Jesús Alcázar¹

• ¹Janssen Research and Development, Janssen-Cilag Department of Medicinal Chemistry S.A., Toledo, Spain
• ²Molecular Design and Synthesis University of Leuven, Department of Chemistry, Heverlee Belgium
• ³Universidad de Castilla-La Mancha Facultad de Ciencias y Tecnologías Químicas Real, Spain

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