3-硝基-2-吡啶亚磺酰基（Npys）保护基的硫解。一种肽合成中通用脱保护方案的方法。
Thiolysis of the 3-nitro-2-pyridinesulfenyl (Npys) protecting group. An approach towards a general deprotection scheme in peptide synthesis.
作者信息
Rosen O, Rubinraut S, Fridkin M
机构信息
Department of Organic Chemistry, Weizmann Institute of Science, Rehovot, Israel.
出版信息
Int J Pept Protein Res. 1990 Jun;35(6):545-9. doi: 10.1111/j.1399-3011.1990.tb00260.x.
The hydroxylic side-chain functional groups of serine, threonine, hydroxproline and tyrosine, the alpha and epsilon-amino moieties of lysine and the thiol group of cysteine were masked by the 3-nitro-2-pyridinesulfenyl (Npys) protecting group. Deprotection was mildly affected by thiolysis with either 2-mercaptopyridine and 2-mercaptomethyl imidazole (O- and N-Npys) or with 3-mercaptoacetic acid and 2-mercaptoethanol (S-Npys). Thiolysis was monitored spectrophotometrically and was completed in a rather short time. Incorporation of the Npys group into a whole and single thiolyzable deprotection scheme is suggested.
丝氨酸、苏氨酸、羟脯氨酸和酪氨酸的羟基侧链官能团、赖氨酸的α和ε-氨基部分以及半胱氨酸的巯基被3-硝基-2-吡啶亚磺酰基（Npys）保护基团所掩盖。用2-巯基吡啶和2-巯基甲基咪唑（O-和N-Npys）或3-巯基乙酸和2-巯基乙醇（S-Npys）进行硫解可温和地实现脱保护。硫解通过分光光度法进行监测，并且在相当短的时间内完成。建议将Npys基团纳入一个完整且单一的可硫解脱保护方案中。
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