Na2CO3-Mediated [3+3] Annulation Reaction of Substituted Benzamidines with 2-Benzylidenemalononitriles: Access to Substituted Pyrimidine-4,6-diamines

An efficient protocol for the synthesis of 2-aryl-5-benzyl-pyrimidine-4,6-diamines from readily available substituted 2-benzyl-idenemalononitriles and substituted benzamidines was developed. This practical protocol provides high value pyrimidine-4,6-diamines in moderate to good yields under simple reaction conditions. This approach also enables some modifications of structurally complex bioactive molecules and exhibits potential applications in medicinal chemistry.

Automated summary

An efficient protocol for the synthesis of valuable pyrimidine-4,6-diamines from readily available compounds has been developed. This method provides moderate to high yields under simple reaction conditions and allows for modifications of complex bioactive molecules, showing potential applications in medicinal chemistry.