Synthesis of cyclic peptide reniochalistatin E and conformational isomers

Here, we report a convenient and efficient synthesis strategy for the total synthesis of cyclic peptide reniochalistatin E and its conformational isomers with 32% overall yield. We found the linear peptide precursor without side chain gave better cyclization yield.

抗肿瘤环八肽Reniochalistatin E的固相合成

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。