Solid-phase synthesis of skeletally diverse benzofused sultams via palladium-catalyzed cyclization

The solid-phase synthesis of sultams from resin-bound amino acids is described. The sulfonylation of the resin-bound primary amines afforded the requisite secondary amines, after which the intramolecular Buchwald–Hartwig-type coupling forms the C–S bond. A final alkylation on the sulfonamides follow...

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Veröffentlicht in:Tetrahedron letters 2011-03, Vol.52 (13), p.1456-1458
Hauptverfasser: Chen, Wenteng, Li, Zhi, Ou, Lili, Giulianott, Marc A., Houghten, Richard A., Yu, Yongping
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Sprache:eng
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Zusammenfassung:The solid-phase synthesis of sultams from resin-bound amino acids is described. The sulfonylation of the resin-bound primary amines afforded the requisite secondary amines, after which the intramolecular Buchwald–Hartwig-type coupling forms the C–S bond. A final alkylation on the sulfonamides followed by cleavage provided the corresponding seven-membered sultams.
ISSN:0040-4039
1873-3581
DOI:10.1016/j.tetlet.2011.01.055