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

Abstract

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%.