Reformatsky and Blaise reactions in flow as a tool for drug discovery. One pot diversity oriented synthesis of valuable intermediates and heterocycles

    • L. Hucka,b
    • M. Bertona
    • A. de la Hozb
    • A. Díaz-Ortizb
    • J. Alcázar*a
    • * Corresponding author
    • a Janssen Research and Development, Janssen-Cilag, S.A., C/ Jarama 75, Toledo, Spain
    • b Facultad de Ciencias Químicas, Universidad de Castilla-La Mancha, Ciudad Real, Spain

    The application of Reformatsky and Blaise reactions for the preparation of a diverse set of valuable intermediates and heterocycles in a one-pot protocol is described. To achieve this goal, a greener activation protocol for zinc in flow conditions has been developed to introduce this metal efficiently into α-bromoacetates. The organozinc compounds were added to a diverse set of ketones and nitriles to obtain a wide range of functional groups and heterocyclic systems.

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