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    • 5. 发明专利
    • Method for producing donepezil
    • 生产二苯乙烯的方法
    • JP2013040150A
    • 2013-02-28
    • JP2011179817
    • 2011-08-19
    • Taiwan Biotech Co Ltd信東生技股▲ふん▼有限公司
    • SHEU KUEN-WANGHUANG SHU-FEN
    • C07D211/32A61K31/445A61P25/28C07B61/00
    • PROBLEM TO BE SOLVED: To provide a novel method for producing donepezil, particularly to shorten the reaction time, reduce the cost, and improve safety.SOLUTION: The method includes a step of mixing E2M, an organic solvent, a weak base, sodium dithionite, and a phase-transfer catalyst to obtain an E2M mixture solution; a step of heating the E2M mixture solution and adding water thereto to obtain a heated E2M aqueous solution having an organic layer; and a step of extracting the organic layer from the heated E2M aqueous solution, condensing and drying the organic layer to obtain donepezil. The use of sodium dithionite as a reducing agent improves the safety of a hydrogen gas used in the conventional method and reduces the cost in contrast to the conventional very high-priced nobel metal catalyst. Furthermore, the method requires only 60 minutes of reaction time to synthesize donepezil with a promising yield of more than 85% and much increases the production efficiency of donepezil and the economical value thereof.
    • 要解决的问题:提供一种制备多奈哌齐的新方法,特别是缩短反应时间,降低成本,提高安全性。 解决方案:该方法包括将E2M,有机溶剂,弱碱,连二亚硫酸钠和相转移催化剂混合以获得E2M混合物溶液的步骤; 加热E2M混合溶液并向其中加水以获得具有有机层的加热的E2M水溶液的步骤; 从加热的E2M水溶液中萃取有机层,冷凝干燥有机层得到多奈哌齐的步骤。 使用连二亚硫酸钠作为还原剂提高了常规方法中使用的氢气的安全性,并降低了与传统的非常高价格的诺贝尔金属催化剂相反的成本。 此外,该方法仅需60分钟的反应时间合成多奈哌齐,产率高达85%,大大提高了多奈哌齐的生产效率及其经济价值。 版权所有(C)2013,JPO&INPIT