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US 2019/0100538 A1Published application
Process for the preparation of baricitinib and an intermediate thereof
AssigneeSun Pharmaceutical Industries Limited
InventorsMd Abul Kalam AZAD, Gyanendra PANDEY, Kaptan SINGH, Mohan PRASAD
Life of this patent
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Abstract
The present invention provides processes for the preparation of baricitinib of Formula I and an intermediate of Formula V. The present invention also provides the use of the intermediate of Formula V for the preparation of baricitinib.
Claims14
1-15. (canceled)
A process for the preparation of {1-(ethylsulfonyl)-3-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1l-yl]azetidin-3-yl}acetonitrile of Formula V,
- comprising the steps of:
- i) reacting tert-butyl 3-(cyanomethylidene)azetidine-1-carboxylate of Formula VI
- with a zeolite to obtain 3-(cyanomethylene)azetidine hydrochloride of Formula VII;
- ii) reacting the 3-(cyanomethylene)azetidine hydrochloride of Formula VII with ethanesulfonyl chloride to obtain 2-(1-(ethyl sulfonyl)azetidin-3-ylidene)acetonitrile of Formula II;
- and
- iii) reacting the 2-(1-(ethylsulfonyl)azetidin-3-ylidene)acetonitrile of Formula II with 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole of Formula VIII
- to obtain {1-(ethylsulfonyl)-3-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile of Formula V.
4 more elements
A compound of Formula V.
Dependencies are inferred from the claim text.