Rapid and efficient synthesis of 2-amino-4H-benzothiazines
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.
Hari
A
Department of Chemistry, University of Rochester, Rochester, New York 14627, USA.
Miller
BL