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Efficient syntheses of 1,2,3,4,4a,5-hexahydro-pyrazino[2,1-c][1,4]benzothiazine-6,6-dioxide
Authors:Ronald C. Bernotas  Rebecca J. Dooley
Affiliation:a Chemical Sciences, Wyeth Pharmaceuticals, 500 Arcola Road, Collegeville, PA 19426 USA
b Discovery Analytical Chemistry, Wyeth Pharmaceuticals, 500 Arcola Road, Collegeville, PA 19426 USA
Abstract:Expeditious routes to 1,2,3,4,4a,5-hexahydro-pyrazino[2,1-c][1,4]benzothiazine-6,6-dioxide, a methylenesulfone-constrained arylpiperazine, have been developed. The key step forms the tricyclic system in a cascade of reactions via a 1,4-addition, nitrogen alkylation, and aromatic substitution sequence.
Keywords:Arylpiperazine   Cascade reaction   Sulfones   Aromatic substitution
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