3 years ago

Discovery of highly functionalized scaffolds: Pyrroloimidazolediones as P2X7 receptor antagonists

Discovery of highly functionalized scaffolds: Pyrroloimidazolediones as P2X7 receptor antagonists
A broad range of pyrroloimidazolediones, new highly functionalized bicyclic heterocycles, was obtained by a cycloaddition reaction between l-pyroglutamide derivatives and Bredereck's reagent. Methanolysis of subsequent pyrroloimidazolediones provided antagonists of P2X7 receptor, with retention of initial stereoconfiguration, with potential applications in the treatment of inflammatory and neurological diseases. We have thus developed a new synthesis of lactamic nitrogen free enaminones which is currently the easiest method cited in the literature to access these compounds.

Publisher URL: www.sciencedirect.com/science

DOI: S0040402017307780

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