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    • 48. 发明申请
    • Method of generating metal chelating affinity ligands
    • 产生金属螯合亲和配体的方法
    • US20060027501A1
    • 2006-02-09
    • US11244603
    • 2005-10-06
    • Lars AnderssonUlf TedebarkTesfai GebruAndreas AxenJean-Luc Maloisel
    • Lars AnderssonUlf TedebarkTesfai GebruAndreas AxenJean-Luc Maloisel
    • B01D15/08
    • B01J45/00B01D15/3828B01J20/286B01J20/3251B01J20/3265C07C323/58C07D333/36
    • The present invention relates to a method of generating at least one polydentate metal chelating affinity ligand, which method comprises the steps of (a) providing at least one cyclic scaffold comprising a carbonyl, an adjacent sulphur and a nucleophile; (b) providing at least one polydentate metal chelating affinity ligand arm, optionally in a form wherein the metal chelating functionalities are protected, on each scaffold by derivatisation of the nucleophile of said scaffolds, while retaining the cyclic structure of the scaffold; (c) ring-opening at the bond between the carbonyl and the sulphur of the derivatised scaffold by adding a reagent that adds one or more metal chelating affinity ligand arms to the scaffold; and, if required, (d) deprotecting the functionalities of the ligand arm(s) provided in step (b). In the most preferred embodiment of the method, steps (c) and (d) are performed simultaneously as one single step.
    • 本发明涉及产生至少一种多齿金属螯合亲和配体的方法,该方法包括以下步骤:(a)提供至少一种包含羰基,相邻硫和亲核试剂的环状支架; (b)在保留支架的环状结构的同时,通过衍生所述支架的亲核试剂,在每个支架上提供至少一种多金属金属螯合亲和配体臂,任选地以金属螯合官能团的形式被保护; (c)通过加入一种将一种或多种金属螯合亲和配体臂添加到支架中的试剂,在衍生化支架的羰基和硫之间的键上开环; 如果需要,(d)使步骤(b)中提供的配体臂的功能脱保护。 在该方法的最优选实施方案中,步骤(c)和(d)同时作为一个步骤进行。