PROCESSES AND INTERMEDIATES FOR MAKING A JAK INHIBITOR

摘要

This invention relates to processes and intermediates for making {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, useful in the treatment of diseases related to the activity of Janus kinases (JAK) including inflammatory disorders, autoimmune disorders, cancer, and other diseases.

主权项

1. A process, comprising:
reacting a compound of Formula III:with a compound of Formula IV:under Suzuki coupling conditions to form a compound of Formula II:wherein:
Z is H or a protecting group; P1 is a protecting group; X1 is halo; and R1 and R2 are each independently H or C1-6 alkyl; or R1 and R2, together with the two oxygen atoms to which they are attached and the boron atom to which the oxygen atoms are attached, form a 5- to 6-membered heterocycloalkyl ring, which is optionally substituted with 1, 2, 3, or 4 C1-4 alkyl groups.