http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-110963928-A

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filingDate 2019-11-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3992d5239305774b98c1b4fe9b55a91a
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publicationDate 2020-04-07-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-110963928-A
titleOfInvention Preparation method of aprepitant intermediate impurity
abstract The invention relates to a preparation method of aprepitant intermediate impurities. The preparation method comprises the following reaction steps: (A) carrying out Grignard reaction on the raw material 1 and Grignard reagent 4-fluorophenyl magnesium halide; (B) carrying out reduction reaction on the reaction product obtained in the step (A) and a reducing agent to obtain a compound 4; (C) carrying out debenzylation reaction on the obtained compound 4 and a deprotection reagent to obtain a crude product 5; (D) reacting the obtained crude product 5 with a protective reagent in the presence of a solvent and alkali to obtain a compound 6; (E) and carrying out deprotection reaction on the obtained compound 6 and acid or alkali in the presence of a solvent, and separating and purifying to obtain a refined product 5. The method of the invention firstly obtains the compound 4 through reduction reaction, and then synthesizes the compound 5 through debenzylation reaction, thus successfully synthesizing the compound 5 and greatly improving the yield and purity of the crude product 5. Further, the crude product 5 is reacted with a protective reagent and purified to obtain a compound 6, and the compound 5 with high purity can be separated through conventional column chromatography after deprotection reaction.
isCitedBy http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-112666279-B
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priorityDate 2019-11-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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