http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-9873706-B2
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_2aa388e460f6cf478bd46c925c6ab10e |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D231-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D205-04 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D205-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D231-10 |
filingDate | 2015-12-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
grantDate | 2018-01-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_646ccea422ef5112d564fc9caf73b699 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_aee99dc88d58da8313367e02130c8f0c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f5d65a4ef92807455d5eec0403b80954 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_40e8ff663b7a7c295c64630ce88029e8 |
publicationDate | 2018-01-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | US-9873706-B2 |
titleOfInvention | Process for the preparation of baricitinib and an intermediate thereof |
abstract | The present invention provides a process for the preparation of baricitinib and an intermediate thereof. The present invention provides a convenient, economical, and industrially advantageous two-step process for the preparation of [4-(IH-pyrazol-4-yl)-7Hpyrrolo[2,3-d] pyrimidin-7-yl]methyl pivalate of Formula (II). The process of the present invention involves the use of an alkali or alkaline earth metal hydroxide, carbonate, or bicarbonate as a base for reacting 4-chloro-7H-pyrrolo[2,3-d]pyrimidine of Formula (III) with chloromethyl pivalate of Formula (IV), and the use of an unprotected pyrazole borolane of Formula (VIII) for the conversion of (4-chloro-7H-pyrrolo[2,3-d] pyrimidin-7-yl)methyl 2,2-dimethylpropanoate of Formula V into [4-(1H-pyrazol-4-yl)-7Hpyrrolo[2,3-d]pyrimidin-7-yl]methyl pivalate of Formula (II). The process of the present invention provides [4-(1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl]methyl pivalate of Formula (I) in high yield. |
isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2020072870-A1 |
priorityDate | 2014-12-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 123.