Imidazolones are pharmaceutically interesting compounds and constitute essential substructures of several receptor antagonists with activities in the low nanomolar regime.[1] Imidazolones are also found in potent PDE4 inhibitors, in subtype selective �3-adrenergic receptor agonists and in GABAA receptor ligands.[1] We here present our results of exploring the chemistry of amino aldehydes in the Pictet-Spengler reaction, in imidazolone formation and subsequent transformations.[1] Figure 1. <img src='https://acs-archive-assets2.s3.amazonaws.com/239nm/uploads/19429_chemistry_for_a_sustainable_world.jpg' alt='' />[1] Diness, F., Meldal, M. Chem. Eur. J. 2009 , 15, 7044 and references cited herein.

Synthesis and functionalisation of imidazolones

243rd National Meeting (2012)

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