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A universal allyl linker for solid-phase synthesis

โœ Scribed by Xiaohu Zhang; Roger A. Jones


Book ID
103406005
Publisher
Elsevier Science
Year
1996
Tongue
French
Weight
133 KB
Volume
37
Category
Article
ISSN
0040-4039

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t-Butyl 6-bromo-(E)-4-hexenoate was used as a handle for the solid-phase synthesis of glycopeptides. The handle was ยฎrst conjugated with Fmoc amino acids to form the allyl esters, which were then attached to the Sieber amide resin via acidic cleavage of the t-butyl esters followed by activation of t

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A range of linkers for the important amidine pharmacophore, cleavable using acid or light have been developed for use in library synthesis. The utility of these linkers is demonstrated by the solid phase synthesis of the Novartis (ex-Ciha) phase II compound CGS-25019C.