The process research and development towards a convergent synthesis of GDC-0853, a reversible Bruton’s Tyrosine Kinase (BTK) inhibitor, will be described. The synthesis includes strategic selection of starting materials and development of a regioselective, catalytic C–N coupling to a linker fragment to assemble the polycyclic target molecule. The multi-kilogram synthesis of the API, control of key impurities and Pd removal will also be discussed.

Development of an expedient synthesis to GDC-0853: A reversible Bruton’s tyrosine kinase inhibitor

253rd National Meeting (2017)

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