Matsueda R, Higashida S, Albericio F, Andreu D
New Lead Research Laboratories, Sankyo Co., Ltd. Tokyo, Japan.
Pept Res. 1992 Sep-Oct;5(5):262-4.
Two recent reports on the partial lability of the 3-nitro-2-pyridinesulfenyl (Npys) thiol protecting group towards 1-hydroxy-benzotriazole (HOBt) have prompted a rechecking of the chemical behavior of this group. Using both soluble and polymer-bound forms of Cys(Npys) as test materials, the complete stability of this protection against HOBt has now been definitively established, and its compatibility with Boc-benzyl-based solid-phase synthesis strategies has been clearly confirmed by stability assays against a wide range of reagents, as well as by the successful synthesis of several Cys(Npys)-containing peptides.
最近有两份报告指出3-硝基-2-吡啶亚磺酰基（Npys）硫醇保护基对1-羟基苯并三唑（HOBt）具有部分不稳定性，这促使人们重新审视该保护基的化学行为。使用可溶性和聚合物结合形式的Cys(Npys)作为测试材料，现已明确确定该保护基对HOBt具有完全稳定性，并且通过针对多种试剂的稳定性测定以及成功合成几种含Cys(Npys)的肽，明确证实了其与基于Boc-苄基的固相合成策略的兼容性。
