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Thionyl chloride-phenol and phosphorus oxychloride-phenol could be used as efficient deprotectio nagents in peptide synthesis

机译:亚硫酰氯 - 苯酚和磷氧化磷酸磷酸磷酸磷酸苯酚可用作肽合成中的有效的去脱离文字

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Hydrogen chloride in organic solvent has long been used for removing t-Boc protection in peptide synthesis [1]. However, this method is limited with its tedious operation and low efficiency. Endeavor to an alternative deprotecting reagent has recently been made by Kaiser and Tam and co-workers [2,3] usign Me_3SiCl-PhOH in DCM. As an attempt to search for cheaper and more convenient deprotecting agnet, SOCL_2PhOH (reagent S) and POCl_3-PhOH(reagent P) were designed in this paepr with the same criteria as Kaiser/Tam's method. Phenol served as proton donor and carbonium ion scavenger, however, Me_3SiCl was replaced by SOCl_2 or POCl_3. Reagents S and P were first tested in model experiments to investigate their deprotecting efficiency, and then were employed in solid phase peptide synthesis (SPPS).
机译:有机溶剂中的氯化氢长期以来已经用于去除肽合成中的T-Boc保护[1]。然而,这种方法受到繁琐的操作和低效率的限制。最近由Kaiser和TAM和Co-Workers作出的替代脱紫外试剂[2,3] USIGN ME_3SICL-PHOH。作为搜索更便宜和更方便的脱保护AGNET的尝试,SOCL_2phoh(试剂S)和POCL_3-PHOH(试剂P)在该PAEPR中设计了与Kaiser / Tam的方法相同的标准。然而,苯酚用作质子供体和碳酸氨基清除剂,但是,ME_3SICL被SOCL_2或POCL_3所取代。首先在模型实验中测试试剂S和P,以研究其脱保护效率,然后用于固相肽合成(SPP)。

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