Abstract
The successful coupling of amino acid derivatives during the synthesis of a peptide by either solution or solid-phase procedures depends on both the reactivity of the carboxyl group of the N-protected amino acid and the steric accessibility of the reactive nucleophile (either a primary or secondary amine). Activation of the carboxyl group is a requisite for the synthesis of an amide bond. Many activation procedures have been developed to accomplish this, and ultimately, the reactivity of the activated species is crucial in determining the coupling yield.
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Pennington, M.W., Byrnes, M.E. (1994). Procedures to Improve Difficult Couplings. In: Pennington, M.W., Dunn, B.M. (eds) Peptide Synthesis Protocols. Methods in Molecular Biology, vol 35. Humana Press, Totowa, NJ. https://doi.org/10.1385/0-89603-273-6:1
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DOI: https://doi.org/10.1385/0-89603-273-6:1
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