The solid-phase synthesis of indolines from resin-bound 2-bromophenylacetylated amino acids is described. The exhaustive reduction of solid-support bound amides with borane afforded the requisite secondary amines that, following the palladium-catalyzed intramolecular cyclization and cleavage, provid
Solid-phase synthesis of skeletally diverse benzofused sultams via palladium-catalyzed cyclization
β Scribed by Wenteng Chen; Zhi Li; Lili Ou; Marc A. Giulianott; Richard A. Houghten; Yongping Yu
- Book ID
- 104098843
- Publisher
- Elsevier Science
- Year
- 2011
- Tongue
- French
- Weight
- 243 KB
- Volume
- 52
- Category
- Article
- ISSN
- 0040-4039
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β¦ Synopsis
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.
π SIMILAR VOLUMES
A new procedure for the solid-phase synthesis of 2,6-and 2,7-diamino-4(3H)-quinazolinones is described. The method involves coupling of 2,4,6-and 2,4,7-trichloroquinazoline to a solid support via benzyl alcohol type linkers, subsequent displacement of chlorine at C-2 then at the C-6 or C-7 positions