Process Development and Large-Scale Synthesis of BTK
Inhibitor BIIB068

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

doi:10.1021/acs.oprd.0c00087.s001

Process Development and Large-Scale Synthesis of BTK Inhibitor BIIB068

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posted on 2020-04-27, 14:15 authored by Chaomin Li, Lloyd 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 M. 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) a streamlined process with significantly improved overall yield, and (3) appropriate impurity control (including potential mutagenic impurities), which enabled delivery of quality material for toxicology studies and clinical trials.

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Large-Scale Synthesis toxicology studies transition metal process optimization quality material BTK Inhibitor BIIB 068 Chemical process development efforts impurity control BIIB 068 hemiadipate multikilogram production process Development

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CC BY-NC 4.0

Process Development and Large-Scale Synthesis of BTK Inhibitor BIIB068

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