Hemiasterlin is a special cytotoxic tripeptide isolated from marine sponges and composed of three special amino acids [1]. Hemiasterlin is a more potent in vitro cytotoxin and antimitotic agent than Taxol or vincristine, and preliminary experiments have demonstrated promising in vivo activity [2,3] The total synthesis or Hemiasterlin was previously reported by several papers using a patented process requiring more than 18 tedious step reactions and generating very low total yield (<5%) [1-3]. Here we report an improved total synthesis route with 13 step reactions and an increased total yield (17%), which allows hundreds of mg of Hemiasterlin to be synthesized at one time.
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