Preparation method of dabigatran etexilate intermediate

• Main Authors: WAN XINQIANG, ZHANG LEI, WANG FUQUAN, ZHONG ZHAOLIANG
• Format: Patent
• Language: Chinese; English
• Published: 13.06.2023
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

The invention discloses a preparation method of a dabigatran etexilate intermediate, which comprises the following steps: putting 0.05 mol of reactant I into a reaction container, adding a solvent for dissolving, adding reactant chloroacetaldehyde, then adding an oxidant, adding a catalyst, reacting at room temperature, separating the product after the reaction is finished, and recrystallizing and purifying to obtain a high-purity product compound II, and reacting the compound II with p-aminobenzonitrile to obtain a dabigatran etexilate intermediate compound III. The method has the beneficial effects that the process is simple, the reaction raw materials are simple and easy to obtain, the reaction condition is mild, the reaction product is convenient to treat, the reaction selectivity is good, the generation of reaction impurities can be effectively reduced, the reaction yield is improved, the product with higher purity is obtained, the atom economy of the reaction is improved, and the method is suitable for