Selective, on-resin N-methylation of peptide N-trifluoroacetamides.
Selective, on-resin N-methylation of peptide N-trifluoroacetamides.
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DOI：
10.1021/ol402341u
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发表时间：
2013-09
期刊：
影响因子：
5.2
通讯作者：
Rushia A. Turner;Niels E Hauksson;Jordan H Gipe;R. Lokey
中科院分区：
文献类型：
--
作者：
Rushia A. Turner;Niels E Hauksson;Jordan H Gipe;R. Lokey
Mild and efficient methods for site-specific methylation of peptide backbone amides are important tools for chemists seeking to modulate the pharmacokinetic properties of peptide drugs. The Mitsunobu reaction was used to selectively methylate N-trifluoroacetamide (Tfa) protected peptides on-resin. The Tfa group was removed quickly and completely by reduction with excess NaBH4, and it was shown to be orthogonal to many of the protecting groups used in solid-phase peptide synthesis.
