HBTU activation for automated Fmoc solid-phase peptide synthesis

Autor: C G, Fields, D H, Lloyd, R L, Macdonald, K M, Otteson, R L, Noble
Rok vydání: 1991
Předmět:
Zdroj: Peptide research. 4(2)
ISSN: 1040-5704
Popis: Excellent results have been obtained for the Fmoc solid-phase syntheses of peptides using the activating reagent 2-(1H-benzotriazol-1-yl)-1,1,3,3,-tetramethyluronium hexafluorophosphate (HBTU). Activation occurs very rapidly in N,N-dimethylformamide and N-methyl-pyrrolidone, optimal solvents for peptide-resin solvation. It has been observed that complete coupling reactions occur in only 10-30 min. Residues such as Arg, Ile, Leu and Val, which often require double coupling by other activation methods, react with high efficiency by single coupling when HBTU is used. The Fmoc/HBTU chemistry has recently been applied to the peptide synthesizers. The incorporation of trityl side-chain protection for Fmoc-Asn and Fmoc-Gln further enhances coupling efficiencies in difficult sequences.
Databáze: OpenAIRE