An efficient synthesis of the novel triazoloquinazoline adenosine antagonist, CGS 15943, is reported in five steps in approximately 50% overall yield. A key reaction in the synthetic sequence is the double cyclization of an N‐(substituted‐2‐cyanophenyl)carbamate with a carboxylic acid hydrazide to afford a [1,2,4]triazolo‐[1,5‐c]quinazolin‐5(6H)‐one in high yield without either a Dimroth or “translocative” rearrangement occurring. Another key reaction is the condensation of a 2‐(1H‐1,2,4‐triazol‐5‐yl)benzenamine with cyanamide under acidic conditions to prepare a guanidine.

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