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Updated: Aug 15, 2026

Preparation of Stable Bicyclic Aziridinium Ions and Their Ring-Opening for the Synthesis of Azaheterocycles
Published on: August 22, 2018
[Synthesis of p-aminobenzenesulfonyldiazine]
Abstract:
New sulfones were synthesized; these are analogues of bis-(4-aminophenyl)sulfone (DDS) but contain, instead of one benzene nucleus, a heterocycle that is a pyrimidine, pyrazine or pyridazine nucleus. This was substituted with amine, methoxy, methyl groups or halogens in order to obtain long-acting drugs, similarly to those obtained in the field of sulfonamides. The synthesis was accomplished by reaction of sodium p-amino- or p-acetamidobenzensulfinate with the corresponding halodiazine; only the p-aminophenyl 3-aminopyridazin-6-yl sulfone was obtained by acid hydrolysis. The compounds showed good antitubercular activity in vitro.
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