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A solid-phase technology for the preparation of combinatorial libraries through amide-bond anchoring
A solid-phase technology for the preparation of combinatorial libraries through amide-bond anchoring
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机译:通过酰胺键锚固制备组合文库的固相技术
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摘要
The present invention provides the means to suppress epimerisation of the C alpha terminal amino acid of a protected peptide sequence during coupling by using the protection moiety shown in (1) which is referred to as a "precursor linker". This moiety has a number of features; the functional group R and the 2-hydroxyl function lie in a para position relative to each other while the ether residue lies in a para position relative to the aldehyde residue. R1 is an electron donating alkyl group. The R group is a moiety that may readily be interconverted between electron-withdrawing and electron donating. This is based on the safety catch principle. The principle, that a stable bond is smoothly converted to a labile one at a convenient point during a synthesis, has been applied in peptide chemistry for the development of linkers and protecting groups. One approach has been to exploit the facile reductive conversion of a sulphoxide to sulphide. This approach when applied to the precursor linker (1) provides the functional protection moieties which are referred to as "linker compounds".
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机译:本发明提供了通过使用(1)中所示的被称为“前体接头”的保护基团来抑制偶联过程中被保护的肽序列的Cα末端氨基酸的差向异构化的方法。该部分具有许多特征。官能团R和2-羟基官能团相对于彼此位于对位,而醚残基相对于醛残基位于对位。 R 1是供电子性烷基。 R基团是可以容易地在吸电子和给电子之间相互转换的部分。这基于安全捕获原则。稳定键在合成过程中的方便点顺利转变为不稳定键的原理已应用于肽化学中,以开发连接基和保护基。一种方法是利用亚砜容易地还原转化为硫化物。当将该方法应用于前体接头(1)时,提供了功能保护部分,其被称为“接头化合物”。
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