Synthesis of a cyclotetradepsipeptide corresponding to the sequence of AM-toxin II (2a) was achieved, using methanesulfonyl chloride containing sulfur dioxide in the final step of dehydration. The peptide obtained was identical with natural 2a in regard to mp, TLC, UV, MS, ORD, crystal form and biological activity. An analog [l-Phe1]-AM-toxin (2b), simultaneously synthesized, showed extremely weak activity.
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Shimohigashi et al. (1977) studied this question.
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