Synthesis method for antibody-coupled drug linker LND1067

The invention provides a synthesis method for an antibody-coupled drug linker LND1067. The synthesis method comprises the following steps: enabling LND1067-L1 and LND1029 to react in a solvent, enabling reaction liquid to pass through a reversed-phase column, and purifying to obtain LND1067-1; react...

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Hauptverfasser: LI HAIHONG, KONG LINGPEI
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention provides a synthesis method for an antibody-coupled drug linker LND1067. The synthesis method comprises the following steps: enabling LND1067-L1 and LND1029 to react in a solvent, enabling reaction liquid to pass through a reversed-phase column, and purifying to obtain LND1067-1; reacting the LND1067-1 with diethylamine in DMF, decompressing the reaction liquid to remove diethylamine, passing through the reversed-phase column, and purifying to obtain LND1067-2; reacting the LND1067-2, LND1067-L2 and N, N-diisopropylethylamine in a reaction solvent, passing through the reversed-phase column to be purified, and obtaining the antibody-coupled drug linker LND1067. The synthesis method disclosed by the invention is high in yield and easy for large-scale production. 本发明提供了一种用于抗体偶联药物连接子LND1067的合成方法。该合成方法包括:将LND1067-L1与LND1029在溶剂中反应,反应液过反相柱,纯化得到LND1067-1;将LND1067-1与二乙胺在DMF中反应,反应液减压除去二乙胺,过反相柱,纯化得到LND1067-2;将LND1067-2、LND1067-L2和N,N-二异丙基乙胺在反应溶剂中反应,反应液过反相柱纯化,得到用于抗体偶联药物连接子LND1067。本发明的合成方法的收率高,易于放大生产。