190595-65-4Relevant articles and documents
METHOD OF PREPARING EZETIMIBE AND INTERMEDIATE THEREOF
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Paragraph 0074-0076, (2019/08/30)
Disclosed is a method of preparing ezetimibe, including cross-metathesis using a Grubbs 2nd catalyst and deprotection using a Pearlman's catalyst, and an intermediate thereof. The method of preparing ezetimibe is useful as an efficient ezetimibe synthesis technique in pharmaceutical fields using ezetimibe as a raw material.
Preparation method of ezetimibe intermediate
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Paragraph 0043; 0046; 0050; 0054, (2018/07/30)
The invention provides a preparation method of an ezetimibe intermediate I. The preparation method includes: (1), in an inert solvent and at the presence of alkali, enabling a compound shown as a formula III to react with fluoroacetophenone to obtain a compound shown as a formula II; (2), providing a mixed solution A of hexamethyl disilicon sodium amide and an organic solvent; (3), enabling the compound shown as the formula II to react with the mixed solution A to obtain a compound shown as a formula I. The method can be completed at room temperature, reaction yield is increased to about 90% from 70% of the prior art, reactant purity is improved greatly, and a condition is provided for realizing industrial production of ezetimibe.
Ezetimibe intermediate, synthesis method of intermediate and synthesis method of ezetimibe
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, (2017/07/01)
The invention provides an ezetimibe intermediate, a synthesis method of the intermediate and a synthesis method of ezetimibe. The method is short in synthetic route. The method includes the steps of making fluorobenzene as the initial raw material sequentially have acylation reaction with glutaric anhydride and 4(S)-4-phenyl oxazolidinone to generate a compound II, protecting carbonyl through 2,2-bis-substituted-1,3-propylene glycol to obtain a compound III, generating a compound V through the compound III and a compound IV under the catalysis of titanium tetrachloride, cyclizing the compound V to generate a compound VI, hydrolyzing the compound VI to obtain a compound VII, and reducing the compound VII through a borane chiral reducing agent and removing a benzyl protecting group in a hydrogenated mode to obtain the ezetimibe. The method is high in yield, little in side reaction and suitable for industrial mass production.