One-pot, four-component sequential synthesis of novel 4-arylamino-5-carboxyl pyrimidine derivatives

Chengyuan Liang, Chunyang Shi,

Abstract

An operationally simple, one-pot, three-step tandem method has been developed to afford 4-arylamino-5-carboxyl pyrimidine derivatives, which engages four reactive substrates (triphosgene, arylamine, ethyl acetoacetate, substituted ureas ) employing triethylamine as catalyst. The key advantages of this unique, atom-economical reaction are short reaction time, high yields, simple workup, purification of products by non-chromatographic methods and avoiding separation of volatile hazardous isocyanate intermediates.