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Selecting optimal operating conditions for coupling reactions, useful e.g. in preparation of pharmaceuticals, particularly selection of catalysts, includes immunological detection of coupled products

机译:选择最佳的偶联反应操作条件,例如在制备药物时,特别是选择催化剂时,包括偶联产物的免疫学检测

摘要

Method for screening the operating conditions for a coupling reaction between at least two functional groups. Method for screening the operating conditions for a coupling reaction between at least two functional groups comprises: (1) reacting at least two compounds, E1-X1-G1 and E2-X2-G2, in solution and under predetermined operating conditions, with at least one being a candidate operating condition (COC), to produce a compound (Z) of formula E1-X1-G1-G2-X2-E2; (2) determining the concentration of (Z) at a predetermined time (t), by at least one immunological assay, using at least one antibody (AC1) specific for the molecule (M1) of which E1 is the residue; and (3) evaluating the effect of one or more COC on the reaction, from the measured concentration of (Z). G1, G2 : first and second functional groups; X1 and X2 : covalent bonds or linkers; E1 : residue of molecule M1 for which a specific antibody (AC1) is available; E2 : residue of second molecule M2 for which a second antibody (AC2) is available, or a group able to form at least one covalent bond with AC1 in presence of a coupling agent An independent claim is also included for a kit for the new process.
机译:筛选用于至少两个官能团之间的偶联反应的操作条件的方法。筛选至少两个官能团之间偶联反应的操作条件的方法包括:(1)使至少两种化合物E1-X1-G1和E2-X2-G2在溶液中和预定的操作条件下与至少一种是候选操作条件(COC),以产生式E1-X1-G1-G2-X2-E2的化合物(Z); (2)使用至少一种对以E1为残基的分子(M1)具有特异性的抗体(AC1),通过至少一种免疫测定法在规定时间(t)求出(Z)的浓度。 (3)从所测的(Z)浓度评估一种或多种COC对反应的影响。 G1,G2:第一和第二官能团; X1和X2:共价键或接头; E1:分子M1的残基,其可获得特异性抗体(AC1); E2:可获得第二抗体(AC2)的第二分子M2的残基,或在偶联剂存在下能够与AC1形成至少一个共价键的基团。该新方法的试剂盒还包括独立权利要求。

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