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Ligation of the N‐terminal tripeptide 15 and C‐terminal dipeptide 26 to yield Cbz‐Azastatin‐OMe, 27. The final deprotection yielded both Azastatin‐OMe, 7 and its N‐ethyl analogue, 28. Reactions and conditions: a) DCM/TFA 1 : 1. b) DCM/TFA 8 : 3. c) DECP, NEt3, DME, 75 % over three steps. d) H2, Pd/C, EtOH, 98 % (mixture of 7 and 28).
