We have developed an efficient method for solid phase peptide synthesis which consists of Nα-selective deprotection by dilute methanesulfonic acid, in situ neutralization, and rapid coupling reaction using benzotriazol-1-yl-oxy-tris(dimethylamino)phosphonium hexafluorophosphate or new 2-(benzotriazol-1-yl)oxy-1, 3-dimethylmidazolidinium hexafluorophosphate. This method was successfully used to synthesize several peptides using a new derivative, Boc-Tyr(Dpp) (Dpp : diphenylphosphinyl) and Boc-Arg(HCI) on a phenacylresin. For this method, we employed a fluoride ion final deprotection strategy based on a two-dimensional orthogonal protection scheme.
我们开发了一种高效的固相肽合成方法,包括用稀
甲磺酸进行 Nα 选择性脱保护、原位中和,以及使用
苯并三唑-1-基氧基-三(二甲基氨基)鏻六氟磷酸盐或新的 2-(苯并三唑-1-基)氧基-1, 3-二甲基
咪唑鎓
六氟磷酸盐进行快速偶联反应。我们在苯甲
树脂上使用新的衍
生物 Boc-Tyr(Dpp)(Dpp:
二苯基膦酰基)和 Boc-Arg(HCI),成功地用这种方法合成了几种肽。在这种方法中,我们采用了基于二维正交保护方案的
氟离子最终脱保护策略。