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    • 9. 发明申请
    • Polymeric compounds
    • 聚合物
    • US20050090651A1
    • 2005-04-28
    • US10491216
    • 2002-09-26
    • Richard SmithJason BetleyDirk Esser
    • Richard SmithJason BetleyDirk Esser
    • C07K1/04C07K1/107C07K14/705C07K14/815C07K14/00C07D279/12
    • C07K14/70596C07K1/047C07K1/1075C07K1/1077C07K14/815
    • The invention provides a process for forming a compound having the formula (I): from chemical entities native [A], native [B] and native [C], where native [A] has a thioester group, native [B] had a 1-amino-2-thiol group with an unoxidised sulfhydryl side chain, and native [C] had a thiol reactive function (TRF) group, wherein chemical entities [A], [B] and [C] are covalently linked by linker group L, comprising the steps of: (i) admixing native [A] and native [B] in a reaction solution; (ii) condensing the unoxidised sulfydryl side chain of native [B] with the thioester group of native [A] for producing a first intermediate compound wherein [A] and [B] are linked with a β-aminothioester bond; (iii) rearranging the β-aminothioester bond for producing a second intermediate compound wherein [A] and [B] are linked with an amide bond having attached thereto a free thiol group; (iv) admixing native [C] with the second intermediate compound in a reaction solution; and (v) reacting the thiol reactive function (TRF) group of native [C] with the free thiol group of the second intermediate compound for producing a compound having the formula (I).
    • 本发明提供了一种用于形成具有式(I)的化合物的方法:从天然[A],天然[B]和天然[C]的化学实体,其中天然[A]具有硫酯基,天然[B]具有 具有未氧化巯基侧链的1-氨基-2-硫醇基团,天然[C]具有硫醇反应性功能(TRF)基团,其中化学实体[A],[B]和[C]通过连接基团共价连接 L,包括以下步骤:(i)将天然[A]和天然[B]混合在反应溶液中; (ii)将天然[B]的未氧化硫辛酸侧链与天然[A]的硫酯基团缩合,以制备其中[A]和[B]与β-氨基硫酯键连接的第一中间体化合物; (iii)重新布置β-氨基硫酯键以制备第二中间体化合物,其中[A]和[B]与附着有游离巯基的酰胺键连接; (iv)将天然[C]与第二中间体化合物在反应溶液中混合; 和(v)使天然[C]的硫醇反应性官能团(TRF)基团与第二中间体化合物的游离巯基反应,以制备具有式(I)的化合物。