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Method for preparing oxytocin antagoniste derivatives, intermediates for the preparation of oxytocin antagonist derivatives and method for preparing the intermediates

机译:催产素拮抗剂衍生物的制备方法,制备催产素拮抗剂衍生物的中间体和制备中间体的方法

摘要

A method for preparing a peptide derivative of formula (I) or a salt thereof: which method comprises the steps of removing two MBzl groups from a compound of formula (II) or a salt thereof: wherein MBzl represents a 4-methoxybenzyl group which serves as a protective group for a thiol group, and R1 and R2 represent hydrogen or a protective group for Trp or Arg respectively; and subsequently oxidizing in an aqueous medium having a pH from 4 to 6 to form an intramolecular disulphide bond; intermediates useful for preparing the compounds of formula (I) and preparation of the intermediates.
机译:一种制备式(I)的肽衍生物或其盐的方法: <图像文件=“ IMGA0001.GIF” he =“ 37” id =“ ia01” imgContent =“ chem” imgFormat =“ GIF” wi =“ 140” /> 哪种方法包括从式(II)化合物或其盐中除去两个MBzl基团的步骤: <图像文件=“ IMGA0002.GIF” he =“ 37” id =“ ia02” imgContent =“ chem” imgFormat =“ GIF” wi =“ 142” /> 其中MBzl代表用作甲硫醇基保护基的4-甲氧基苄基,R 1 和R 2 分别代表氢或Trp或Arg的保护基。随后在pH为4至6的水性介质中氧化以形成分子内二硫键;用于制备式(I)化合物和中间体制备的中间体。

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