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    • 1. 发明申请
    • SYNTHESES OF AZAPEPTIDES BY THE FMOC/TERT-BUTYL/POLYAMIDE TECHNIQUE
    • 通过FMOC /叔丁基/多胺技术合成腈肟酸
    • WO1995008561A1
    • 1995-03-30
    • PCT/GB1994002103
    • 1994-09-26
    • MEDICAL RESEARCH COUNCILJOHNSON, TonyQUIBELL, Martin
    • MEDICAL RESEARCH COUNCIL
    • C07K01/04
    • C07K1/04C07C271/12
    • Disclosed is a method of synthesising a peptide comprising at least one aza-amino acid residue, the method comprising: coupling one or more amino acids to a solid phase support so as to form a supported moiety; activating the supported moiety; reacting the activated supported moiety with one or more aza-amino acid precursors having a fluorenylmethoxycarbonyl (Fmoc)-protected free amino function, so as to form a supported azapeptide; releasing the azapeptide from the solid phase support and deprotecting (if necessary) the side chains of the one or more amino acid and one or more aza-amino acid residues, together with certain novel compounds of use in the method and more generally.
    • 公开了一种合成包含至少一个氮杂 - 氨基酸残基的肽的方法,所述方法包括:将一个或多个氨基酸偶联到固相载体上以形成负载部分; 活化支持的部分; 使活化的支持部分与一种或多种具有芴基甲氧基羰基(Fmoc)保护的游离氨基官能团的氮杂 - 氨基酸前体反应,以形成负载的氮杂肽; 从固相载体中释放azapeptide,并将一个或多个氨基酸和一个或多个氮杂氨基酸残基的侧链(如果需要)脱保护(连同某些在该方法中使用的新化合物)。