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A new copper-catalyzed one-pot reaction resulted in the practical synthesis of imidazolinones in moderate yields from esters. The use of inexpensive copper iodide as the catalyst, (NH4)2CO3 as the nitrogen source and readily available starting materials makes this process economically viable. Applying this protocol to the synthesis of GSK2137305, a concise approach was developed to obtain GSK2137305 from the ester in only three steps with an overall yield of 26.9%.

Graphical abstract: Novel one-pot synthesis of imidazolinones from esters: a concise synthesis of GSK2137305

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