Process Development and Large-Scale Synthesis of BTK Inhibitor BIIB068

Chaomin Li,Lloyd Charles Franklin,Robbie Chen,Tamera Mack,Michael Humora,Bin Ma,Brian T. Hopkins,John Guzowski,Fengmei Zheng,Michael MacPhee,Yiqing Lin,Steven Ferguson,Daniel Patience,George A. Moniz,William F. Kiesman,Erin O’Brien

Process Development and Large-Scale Synthesis of BTK Inhibitor BIIB068

2020

Chaomin Li
Lloyd Charles Franklin
Robbie Chen
Tamera Mack
Michael Humora
Bin Ma
Brian T. Hopkins
John Guzowski
Fengmei Zheng
Michael MacPhee
Yiqing Lin
Steven Ferguson
Daniel Patience
George A. Moniz
William F. Kiesman
Erin O’Brien

Chemical process development efforts leading to multikilogram production of BIIB068 hemiadipate are discussed. Process optimization resulted in (1) removal of transition metal from the process, (2)...

Keywords:

Amination
Combinatorial chemistry
process development
Process optimization
Chemistry
Bruton's tyrosine kinase
Organic chemistry
Transition metal

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