抗肿瘤环八肽Reniochalistatin E的固相合成

Solid-phase Synthesis of Antitumor Cyclic Octapeptide Reniochalistatin E

以2-氯三苯基氯树脂(CTC)为载体,以HCTU/DIPEA为缩合体系,通过Fmoc固相合成法合成直链肽,液相环合,得环肽粗品。制备液相进行纯化。通过HPLC、MS及NMR进行表征分析,目标产物纯度大于98%,总收率为24%。本法操作简便易行,适合该系列环肽的合成。

Antitumor cyclic octapeptide reniochalistatin E was synthesized in this paper. The peptide chain was synthesized by Fmoc solid-phase synthesis using 2-chlorotriphenyl chloride resin(CTC) as the carrier and HCTU/DIPEA as the condensation system, and the peptide chain was cyclized in liquid phase to obtain a crude product. Then it was purificated through preparative liquid chromatograph. The HPLC, MS and NMR was used to characterized the pure product. The results showed that the purity of target product was over 98% and the total yield was 24%. The method was suitable for the synthesis of the series of this kind of cyclic peptides.