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Org Lett. 2000 Nov 16;2(23):3667-70.

Rapid and efficient synthesis of 2-amino-4H-benzothiazines

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  • 1Department of Chemistry, University of Rochester, Rochester, New York 14627, USA.


The benzothiazine nucleus is a relatively unexplored class of compounds, from the standpoint of both synthetic chemistry and biological activity. We have developed a rapid, high-yielding synthesis of benzothiazines in which a precursor aryl thiourea is prepared on solid phase. Addition of trifluoroacetic acid catalyzes a conjugate addition reaction to form the desired heterocycle and releases it from the resin.

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