首页> 外国专利> Procedure for the rapid Synthesis of a Peptide in Solution methods for the synthesis of Combinatorial Libraries of peptides and to the automated Synthesis of peptides in solution that apply this procedure and a Peptide or a Peptide mixture thus obtained (a)

Procedure for the rapid Synthesis of a Peptide in Solution methods for the synthesis of Combinatorial Libraries of peptides and to the automated Synthesis of peptides in solution that apply this procedure and a Peptide or a Peptide mixture thus obtained (a)

机译:在溶液中快速合成肽的方法用于合成肽的组合文库的方法,以及用于在溶液中自动合成肽的方法,该方法应用此程序以及由此获得的肽或肽混合物(a)

摘要

A procedure for the rapid Synthesis of a Peptide in Solution, which involves repeated Cycles of the steps (a) - (d): (a) a phase coupling using an excess of one component to acilar amino carboxylic activated Component, (b) a phase of extinction that uses an agent Sweeper for removing functions carboxu00edlicas activated SewageDone Agent Sweeper can also be used for the Protection of the Peptide in Growth.(c) one or more aqueous Extracts and Optionally, (d) a separate deprotection step, followed by one or more aqueous extractions, where the procedure includes at least one Stage (stage b), called (B '), in which an Amine or thiol which comprises an anion anion free or Latent Sweeper is used as an agent of the functions carboxu00edlicas activated sewage.The anion present in the Amine Sweeper has a temporary Protective Group, Benzyl type, More specifically a protected amino acid derivative in the C - terminal, such as the Beta Alanine. The Sweeper is a Beta alaninate Agent benzyl thiol anion, comprising a Polyamine or a free or Latent.The Procedure includes extraction is carried out in the presence of Sodium Chloride or Potassium nitrate. During the procedure the Peptide on Growth need not be isolated until it has obtained the final sequence of the peptide. This procedure is useful for highly efficient production of oligo - and polypeptides of high purity.Also disclosed are methods for the synthesis of Combinatorial Libraries of peptides and to the automated Synthesis of peptides in solution to apply the procedure and a Peptide or a Peptide mixture thus obtained (a).
机译:一种在溶液中快速合成肽的方法,该方法涉及步骤(a)-(d)的重复循环:(a)使用过量的一种组分与氨基氨基羧酸活化的组分进行相偶联,(b)a使用灭虫剂清除功能的灭绝阶段,也可以使用羧激活的SewageDone灭虫剂来保护生长中的肽。(c)一种或多种水性提取物,以及(d)单独的脱保护步骤,随后进行一次或多次水萃取,其中程序包括至少一个阶段(阶段b),称为(B'),其中将包含无阴离子或潜伏性清扫剂的胺或硫醇用作该功能的试剂胺清扫器中存在的阴离子具有一个临时保护基(苄基型),更特别的是在C端具有一个受保护的氨基酸衍生物,例如β丙氨酸。所述清扫剂是β-丙氨酸盐试剂苄基硫醇阴离子,其包含多胺或游离或潜在的。所述方法包括在氯化钠或硝酸钾的存在下进行萃取。在该过程中,直到获得肽的最终序列才需要分离生长肽。该方法对于高效生产高纯度的寡核苷酸和多肽是有用的。还公开了用于合成肽的组合文库的方法以及用于在溶液中自动合成肽以应用该方法的方法以及由此形成的肽或肽混合物。获得(一)。

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