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Considering the biological and chemical relevance of guanidine containing derivatives, we have devised a novel and efficient two-step synthesis of 2-arylamino-1,4,5,6-tetrahydropyrimidines. We have found that the coupling of aryl bromides with 2-aminopyrimidine is a very effective method for the high yielding synthesis of 2-arylaminopyrimidines. Moreover, the employment of Pd-catalysed hydrogenation to selectively reduce the pyrimidine ring generates a very highyielding pathway to 2-arylamino-1,4,5,6-tetrahydropyrimidines of biological interest.

Synthesis of cyclic guanidines: 2-arylamino-1,4,5,6-tetrahydropyrimidines