Efficient syntheses of 1,2,3,4,4a,5-hexahydro-pyrazino[2,1-c][1,4]benzothiazine-6,6-dioxide |
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Authors: | Ronald C. Bernotas Rebecca J. Dooley |
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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 |
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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. |
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Keywords: | Arylpiperazine Cascade reaction Sulfones Aromatic substitution |
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