Tirapazamine (CAS NO.: ), with its systematic name of 1,2,4-Benzotriazine, 3-amino-, 1,4-dioxide, could be produced through many synthetic methods.

Following are some of the synthesis routes:
1). (I) is condensed with cyanamide disodium salt (II) in hot methanol/water to produce Tirapazamine.
2). 2-Nitroaniline (III) is condensed with cyanamide (IV) by heating at 100 C to afford 3-amino-1,2,4-bezotriazine 1-oxide (V), which is then oxidized with 30% aqueous H₂O₂ in hot acetic acid.
3). 3-Hydroxy-1,2,4-benzotriazine 1-oxide (VI) reacts with refluxing POCl₃ and dimethylaniline to give 3-chloro-1,2,4-benzotriazine 1-oxide (VII), which by reaction with dry ammonia in ethanol is converted into the corresponding amino derivative (V), already obtained.