肿瘤放射性受体显像剂奥曲肽的固相合成

Methodology for Solid Phase Synthesis of Octreotide

  • 摘要: 采用苏氨酸转变为苏氨酸乙酯,再用LiAlH4还原该乙酯合成了苏氨醇,用自动多肽合成仪和Fmoc(9-芴甲基羰基)保护的氨基酸合成了7肽—树脂;再用三氟醋酸铊(Tl(Tfa)3)在7肽—树脂上形成7肽的二硫键;用苏氨醇氨解法裂解肽—树脂并在7肽链上接上苏氨醇形成八肽;然后用三氟乙酸脱去氨基酸侧链保护基团,用高效液相色谱法纯化八肽,得到了奥曲肽(OCT)。

     

    Abstract: The 7 peptide-resin is synthesized by polypeptide synthesizer and Fmoc protected amino acid. The disulfide formation is performed by Tl(Tfa)_3 on the 7 peptide-resin. The side chain protected peptide is cleaved from resin by aminolysis with threoninol. At the same time threoninol is linked to the cleaved peptide. The side chain protective groups is removed by using trifluoroacetic acid(TFA), and the crude linear peptide is purified using HPLC.

     

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