Rink酰胺(RAM)树脂

Rink Amide (RAM) Resins ChemFiles Volume 3 Article 4

已经开发了多种4-((2,4-二甲氧基苯基)(芴甲氧羰基-氨基)甲基)苯氧基烷基官能化载体用于合成肽羧酰胺。(1, 2) 通过用95%的三氟乙酸(TFA)处理可以从这些广泛使用的载体上分离肽酰胺。苄基苯基醚键对高浓度TFA的不稳定性与从原始Rink酰胺树脂4 -((2,4-二甲氧基苯基)(芴甲氧羰基氨基)甲基)苯氧基甲基聚苯乙烯最终裂解过程的副产物形成有关。因此,我们提供的所有Rink酰胺树脂均用改性的Rink酰胺(RAM)连接基团:4-((2,4-二甲氧基苯基)(芴甲氧羰基-氨基)甲基)苯氧基乙酸。(2) 用RAM连接基团酰化的氨甲基聚苯乙烯,也被称为“Knorr”树脂,是肽酰胺SPPS的优秀工具。C-末端氨基酸残基可以使用标准的酰胺形成方法偶联,使用二异丙基碳二亚胺/羟基苯并三唑(HOBt)或脲盐或鏻盐如TBTU或BOP。使用N-烷基Rink树脂可以提供N-烷基酰胺肽。(3)

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参考文献

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