Baricitinib (LY3009104) is a JAK 1/2 inhibitor currently being evaluated in late phase clinical trials at Eli Lilly and Company for treatment of rheumatoid arthritis. As part of the development effort toward the synthesis of the title compound, a scalable route was needed to prepare the penultimate intermediate. Process development was conducted with special emphasis on catalyst selection, solvent selection, and crystallization optimization. In addition, the concepts of process modeling based on the proposed reaction mechanism, and process risk assessment were utilized to ensure reproducible performance on a manufacturing scale.

Process development/optimization on the synthesis of an intermediate leading to baricitinib (LY3009014)

250th National Meeting (2015)

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