A Green, Facile, and Straightforward Synthesis of Pyrimidine‐2,4(1 H ,3 H )‐Diones From tert ‐Butyl (2‐Cyano Aryl/Heteroaryl) Carbamates: A Versatile Approach to Medicinally Relevant Scaffolds

We present a mild and efficient method for the synthesis of diversely substituted pyrimidine‐2,4(1 H ,3 H )‐dione via base‐mediated cyclization of tert ‐butyl (2‐cyano aryl/hetroaryl)carbamates. Our method uses readily available Boc‐protected o ‐aminonitriles and proceeds under basic conditions at 80 °C delivering products in excellent yields. This strategy exhibits broad substrate scope tolerating a wide range of aromatic and heteroaromatic systems with diverse functional groups. Importantly, this approach enables the high‐yield synthesis of lumazine and provides key intermediates for medicinally important compounds including alfuzosin, terazosin, prazosin, IAAP, and doxazosin. This simple, efficient and versatile strategy offers a practical solution for many synthetic and medicinal chemistry challenges.