One synthesis of this compound involves initial alkylation of methyl testosterone by means of strong base and methyl iodide to afford the 4,4-dimethyl derivative. Formylation with alkoxide and methyl formate leads to the 2-hydroxymethyl derivative. Reaction of this last with hydroxylamine leads to formation of an isoxazole ring. There is then obtained azastene.
^Liu, CG; Dai, MZ; Li, WK; Liu, GM; Lin, ZM; Ma, RH (1987). "Interceptive action of azastene and its effects on plasma progesterone in pregnant rats and rabbits". Zhongguo yao li xue bao = Acta pharmacologica Sinica8 (6): 540–3. PMID3451668.