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
MANUFACTURING METHOD OF (3R,4S)-1-(4-FLUOROPHENYL)-[3(S)-HYDROXY-3-(4-FLUOROPHENYL)PROPYL]-[4-(PHENYLMETHOXY)PHENYL]-2-AZETIDINONE
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, (2017/11/18)
PROBLEM TO BE SOLVED: To provide a method for effectively manufacturing high purity (3R,4S)-1-(4-fluorophenyl)-[3(S)-hydroxy-3-(4-fluorophenyl)propyl]-[4-(phenylmethoxy)phenyl]-2-azetidinone with reduced contents of specific impurities and enantiomers. SOLUTION: When a benzyl protective body is manufactured by reacting a benzyl protective keto body and borane in presence of a CBS catalyst, the benzyl protective keto body is injected under a condition with co-existing a part of borane of needed amount in a reaction system in advance and remaining borane is added later to conduct the reaction. SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT