Generally, synthetic schemes that begin with ketones () involve conversion of the ketone with the desired substituents to diaziridines (). These diaziridenes are then subsequently oxidized to form the desired diazirines.
Diaziridines can be prepared from ketones by oximation, followed by tosylation (or mesylation), and then finally by treatment with ammonia (). Generally, oximation reactions are performed by reacting the ketone with hydroxylammonium chloride () under heat in the presence of a base such as pyridine. Subsequent tosylation or mesylation of the alpha-substituted oxygen with tosyl or mesyl chloride in the presence of base yields the tosyl or mesyl oxime. The final treatment of the tosyl or mesyl oxime with ammonia produces the diaziridine. 
Diaziridines can be also produced directly by the reaction of ketones with ammonia in the presence of an aminating agent such as a monochloramine or hydroxyl amine O-sulfonic acid.
Diaziridines can be oxidized to diazirines by a number of methods. These include oxidation by chromium-based reagents such as the Jones oxidation, oxidation by iodine and triethylamine, oxidation by silver oxide, oxidation by oxalyl chloride, or even electrochemical oxidation on a platinum-titanium anode.