The present invention relates to a preparation method of a long-chain compound, which includes the following steps: (1) carrying out condensation reaction on H—R2 and R5N-Glu(OR4)—OR3, wherein, R3 is a carboxyl protecting group, R4 is a carboxyl activating group, and R5 is an amino protecting group; obtaining a compound of formula II; (2) removing carboxyl protecting group R3 and amino protecting group R5 of the compound shown in formula II to obtain a compound of formula III; (3) carrying out condensation reaction on the compound shown in formula III and
to obtain a compound shown in formula I. The method reduces the time of deprotection, and all the reactions can be carried out in a solvent with low boiling point. The post-processing requires only simple washing and recrystallization to obtain the product with higher purity, so the method is suitable for large-scale production.
本发明涉及一种长链化合物的制备方法,包括以下步骤:(1) 对 H-R2 和 R5N-Glu(OR4)-OR3 进行缩合反应,其中,R3 是羧基保护基团,R4 是羧基活化基团,R5 是
氨基保护基团;得到式 II 的化合物; (2) 去除式 II 所示化合物的羧基保护基团 R3 和
氨基保护基团 R5,得到式 III 的化合物; (3) 对式 III 所示化合物和 R5N-Glu(OR4)-OR3 进行缩合反应,其中,R3 是羧基保护基团,R4 是羧基活化基团,R5 是
氨基保护基团。
得到式 I 所示化合物。该方法缩短了脱保护时间,所有反应均可在低沸点溶剂中进行。后处理只需简单的洗涤和重结晶即可得到纯度较高的产品,因此该方法适合大规模生产。