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Solid-phase synthesis of skeletally diverse benzofused sultams via palladium-catalyzed cyclization |
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| Authors: | Wenteng ChenZhi Li Lili OuMarc A. Giulianott Richard A. HoughtenYongping Yu |
| Affiliation: | a Institute of Materia Medica, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, PR China b Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St. Lucie, FL 34987, USA |
| Abstract: | 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. |
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