Phakellistatin 13 is a cycloheptapeptide isolated from sponge and show good suppression action to human hepatoma BEL-7404 cell line. We synthesized Phakellistatin 13 the first time by solution method combination of stepwise coupling and segment condensation and the final deprotection and cyclization were achieved according to our designed method, which was different from the reported process. Comparison of the natural and synthetic specimens of phakellistatin 13 by ¹H and ¹³C NMR spectra gave identical NMR signals. The total synthesis of phakellistatin 13 is significant to further study its derivatives and develop novel antitumor drugs.

Key words: Phakellistatin 13, cyclopeptide, solution-phase, total synthesis