Axinastatin 4 from a marine sponge was synthesized by high-dilution BO
P-Cl cyclization of Trp-Val-Pro-Leu-Thr-Pro-Leu in 94% yield (only 2.5
% at normal dilution), showing the configurations of the last three am
ino acids to be S. Synthetic axinastatin 4 was devoid of cytostatic ac
tivity.