Sun Pharmaceutical Industries Limited

Gyanendra Pandey

Mohan Prasad

Kaptan Singh

Md Abul Kalam Azad

Javeena

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. 

Process for the preparation of baricitinib and an intermediate thereof

The present invention provides a crystalline form of baricitinib characterized by an XRPD pattern substantially as depicted in FIG., a process for its preparation, a pharmaceutical composition comprising it, and its use for the treatment of JAK-associated diseases.

Crystalline form of baricitinib

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.

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Faridabad, India

Gyanendra Pandey