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ADDITIVE FOR PEPTIDE SYNTHESIS SOLVENT AND SYNTHESIS OF PEPTIDE USING THE SAME ADDITIVE

机译:肽合成溶剂的添加剂和使用相同添加剂的肽合成

摘要

PURPOSE:To obtain an additive for adding to a solvent and peptide synthetic method using the above-mentioned additive in order to prevent elimination of a protective group bound to an amino group in peptide synthesis. CONSTITUTION:The objective additive is at least one kind of additive selected from 1-hydroxybenzotriazole, N-hydroxysuccinic imide and 3-hydroxy-3,4- dihydro-4-oxo-1,2,3-benzotriazine. When an carboxyl group in the first amino acid in which an amino group is bound to a protective group is combined with an amino group in the second amino acid to synthesize a peptide, the additive is added to a Lewis base solvent which dissolves the first amino acid to prevent the amino group from elimination from the protective group. Since side reaction can be prevented without eliminating the protective group even when an amino acid bound to the protective group is allowed to stand in the solvent for a long time, as shown in synthesis of a long-chain peptide or peptide synthesis using a wholly automatic synthetic machine, a peptide having high purity can be obtained.
机译:用途:获得用于添加至溶剂的添加剂和使用上述添加剂的肽合成方法,以防止在肽合成中消除与氨基结合的保护基。组成:目标添加剂是至少一种选自1-羟基苯并三唑,N-羟基琥珀酰亚胺和3-羟基-3,4-二氢-4-氧代-1,2,3-苯并三嗪的添加剂。当其中结合有氨基的保护基的第一个氨基酸中的羧基与第二个氨基酸中的氨基结合以合成肽时,将添加剂添加到溶解第一个氨基的路易斯碱溶剂中酸以防止氨基从保护基团消除。如长链肽的合成或使用全自动方法进行的肽​​合成所示,即使使与保护基结合的氨基酸长时间在溶剂中也可以在不消除保护基的情况下防止副反应。通过合成机,可以获得具有高纯度的肽。

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