Facile Synthesis of 4H-1,2,4-Benzothiadiazine-1,1-dioxides

o-Bromoarylsulfonylated amidines prepared either by acylation of amidine with o-bromoarylsulfonyl chloride or through the reaction of o-bromoarylsulfoamide with lactime ether underwent Cu(I)-catalyzed intramolecular cyclization to give 4H-1,2,4-benzothiadiazine-1,1-dioxides in good yield. By varying substituents on arylsulfonyl moieties, amidines, and lactime ethers, a small library of structurally diverse 4H-1,2,4-benzothiadiazine-1,1-dioxide derivatives was prepared.

Cherepakha A.; Kovtunenko V. O.; Tolmachev A.; Lukin O.; Nazarenko K. G.
Synth. Commun. 2011, 41 (13), 1977-1989
DOI: 10.1080/00397911.2010.494815