934245-14-4Relevant articles and documents
Synthesis method of ezetimibe
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Paragraph 0023; 0024, (2016/10/31)
The invention discloses a synthesis method of ezetimibe, which comprises the following steps: under the protection of inert gas, adding N,O-dimethylhydroxylamine hydrochloride and EZE-5 into a solvent, and dropwisely adding a DEAC toluene solution to react, thereby obtaining EZE-15; adding magnesium chips and THF (tetrahydrofuran), and dropwisely adding a 4-fluorobromobenzene THF solution to obtain oily EZE-8; adding ethyl benzene, and stirring; dropwisely adding a prepared triethylamine-formic acid mixed reagent, and adding a catalyst to react, thereby obtaining EZE-9; adding THF and EtOH, stirring, adding 5% Pd/C, replacing air in a reaction bulb with high-purity nitrogen, introducing high-purity hydrogen, and carrying out LC until the reaction is complete, thereby obtaining a crude product EZE-10; and refining the crude product with isopropanol and water to obtain the white crystalline powder high-purity EZE-10. The method has the advantages of high synthesized ezetimibe purity, simple used equipment, simplified steps and low production cost, and is suitable for industrial production.