Synthesis of a New Series of 4-Quinazolinyl Piperazine Aryl Ureas

A convenient and efficient synthetic approach to prepare a novel series of 4-quinazolinyl piperazine aryl ureas is reported involving a convergent route. The key intermediate 4-(1-piperazinyl)-quinazoline was produced from methyl anthranilate chlorination reaction with ter t-butyl 1-piperazinecarboxylate, and amine deprotection. On the other hand, a series of amines were transformed into isocyanates by triphosgene. Without separation, these isocyanates were treated with 4-quinazolinyl-piperazine to generate a range of final products. The synthesis was simple, the products were easy to separate, and the yields were good