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.
METHOD FOR PRODUCING DIPHENYL AZETIDINE DERIVATIVE
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Paragraph 0028; 0030, (2018/07/31)
PROBLEM TO BE SOLVED: To provide a highly efficient industrial production method of a diphenyl azetidine derivative which is a production raw material of a β-lactam derivative useful for the treatment and prevention of hypercholesterolemia such as arteriosclerosis. SOLUTION: There is provided a method for producing a compound represented by the general formula (III) [wherein, R is the same as the case of the general formula (I)] by reacting a compound represented by the general formula (I) [wherein, R represents a lower alkyl group which may be branched, an ally group, a lower alkyl group including a lower alkoxy group, a lower alkyl group including a lower thioalkyl group, a tetrahydropyranyl group, a triphenylmethyl group, a silyl group having a substituent, a phenyl group which may have a substituent and a benzyl group which may have a substituent.] and a compound represented by the general formula (II) [wherein, M represents MgCl, MgBr, MgI or Li) in a toluene solvent. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
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.
