Fields C G, Lloyd D H, Macdonald R L, Otteson K M, Noble R L
Applied Biosystems Inc., Foster City, CA 94404.
Pept Res. 1991 Mar-Apr;4(2):95-101.
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.
使用活化试剂2-(1H-苯并三唑-1-基)-1,1,3,3-四甲基脲六氟磷酸盐（HBTU）进行Fmoc固相肽合成已取得了优异的成果。在N,N-二甲基甲酰胺和N-甲基吡咯烷酮（肽-树脂溶剂化的最佳溶剂）中，活化反应进行得非常迅速。据观察，完全偶联反应仅需10 - 30分钟即可完成。诸如Arg、Ile、Leu和Val等残基，通常需要通过其他活化方法进行双重偶联，而使用HBTU时通过单次偶联就能高效反应。Fmoc/HBTU化学方法最近已应用于肽合成仪。对Fmoc-Asn和Fmoc-Gln采用三苯甲基侧链保护可进一步提高困难序列中的偶联效率。
