Fully Automated Continuous Flow Synthesis of Highly Functionalized Imidazo [1,2-a] Heterocycles

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Org. Lett., Vol. 12, No. 3, 2010

  • Ananda Herath, Russell Dahl, and Nicholas D. P. Cosford*
  • Program in Apoptosis and Cell Death Research and Conrad Prebys Center for Chemical Genomics, Burnham Institute for Medical Research, 10901 North Torrey Pines Road, La Jolla, California 92037

This synthesis was performed using the Syrris Africa (replaced by the Asia system in 2012).

Fully Automated Continuous Flow Synthesis of Highly Functionalized Imidazo[1,2-a] Heterocycles

Abstract: The first continuous flow synthesis of imidazo [1,2-a]pyridine-2-carboxylic acids directly from 2-aminopyridines and bromopyruvic acid has been developed, representing a significant advance over the corresponding in-flask method. The process was applied to the multistep synthesis of imidazo [1,2-a]pyridine-2-carboxamides, including a Mur ligase inhibitor, using a two microreactor, multistep continuous flow process without isolation of intermediates.

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This paper was performed on the Africa system, replaced by the Asia system in 2012.