Continuous flow thermolysis of azidoacrylates for the synthesis of heterocycles and pharmaceutical intermediates

    • Alexander G. O'Brien
    • François Lévesque
    • Peter H. Seeberger
    • Max Planck Institute of Colloids and Interfaces, Potsdam, Germany

    An efficient, safe and scalable procedure for the continuous flow thermolysis of azidoacrylates to yield indoles has been developed and was applied to the synthesis of related heterocycles. The scalability of the process was demonstrated in the continuous flow synthesis of a precursor to the DAAO inhibitor 4H-furo[3,2-b]pyrrole-5-carboxylic acid.

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