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The solid‐phase synthesis of six novel analogues of Kahalalide F (KF), a natural product currently undergoing Phase II clinical trials, is reported. In all these compounds, amides were used as isosteres for the depsi bond. For two of these compounds, we performed an efficient synthesis of N‐Fmoc‐protected (2R,3R)‐2‐amino‐3‐azidobutanoic acid, precursor of the aza‐threonine. This is the first example...
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