http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-9873706-B2

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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
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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

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