Practical total syntheses of axinastatins 2 2b and 3 2c were completed by employing Fmoc protection for the N-terminal, and tert-butyl ester blocking for the C-terminal, units of the amlno add and peptide intermediates. Generally, diethyl phosphorocyanidate proved effective for formation of the peptide bond, and in the one exception, asparagine, the o-nitrophenyl active ester proved to be useful. For the final cyclization reaction BOP-Cl was found especially effective.
|Original language||English (US)|
|Number of pages||6|
|Journal||Journal of the Chemical Society - Perkin Transactions 1|
|State||Published - Oct 7 1996|
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