Predicate |
Object |
assignee |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_2578b4fd6a6f637abccee553ab3d936d http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_12332f9bb40abf3752ef706f5e3b5160 |
classificationCPCAdditional |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C2603-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07B2200-07 |
classificationCPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C213-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C213-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C213-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C269-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C213-10 |
classificationIPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C271-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C269-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C213-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C213-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C213-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C213-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C217-10 |
filingDate |
2019-11-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3992d5239305774b98c1b4fe9b55a91a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_654b92a6ccfcd61815cf34b03e5797dd http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b17eee1494f996ce0d624860dc730c21 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_14875b3adf5c1dae0847ea99904efd37 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_66c38a3b1733d98508138eecc17377a8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5a55d0d6b18be6d4294ec8779898f350 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6b305edeeeeeb970385e89b7480540d0 |
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 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-112666279-A |
priorityDate |
2019-11-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type |
http://data.epo.org/linked-data/def/patent/Publication |