Method for large-scale preparation of tafluprost

• Main Authors: HUANG JINLONG, JIANG XIAOMENG, PANG XIONG, LIN JUN, NI LEPING, XU CHUNLIU, ZONG YUEXI, SHI CUNYUAN
• Format: Patent
• Language: Chinese; English
• Published: 12.01.2021
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; METALLURGY; ORGANIC CHEMISTRY

The invention discloses a method for industrially preparing tafluprost. The method comprises the following steps: taking Corey lactone as an initial raw material, oxidizing, condensing, fluorinating,deprotecting, reducing, re-condensing, esterifying and refining to obtain the tafluprost, according to the method for large-scale preparation of the tafluprost provided by the invention, a reversed-phase and normal-phase preparative column purification technology is used, a molecular group evacuation technology is adopted, and a molecular group'evacuation agent 'is added into a mobile phase, so that a relatively good effect is achieved, in addition, a trichloroacetonitrile uric acid(TCCA)reagent is adopted in an oxidation method, and the yield of the tafluprost is improved. The use of variousreaction quenching agents is also the characteristic of the method, and the timely and reasonable quenching of the reaction has certain significance for reducing the generation of impurities. 本发明公开了一种他氟前列素工业化制备的方法，其包括以下步骤：以科立内