FIELD: chemical technology, organic chemistry. SUBSTANCE: invention relates to the improved method of synthesis of N-(8-methoxy-5-quinolinesulfonyl)-aziridine (I) without use of toxic ethyleneimine. Synthesized is carried out from 8-methoxy-5-quinolinesulfochloride (II) that is converted through 8-methoxy-5-[N-(2-hydroxyethyl)] -quinolinesulfonamide (III) to 8-methoxy-5-[N-(2-chloroethyl)] -quinolinesulfonamide (IV) that is cyclized to compound (I) by effect of alkaline metal hydroxides in an aqueous solution at usual temperature according the following scheme: 
(IVI to 
(I). EFFECT: improved method of synthesis.
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