Process Development and Large-Scale Synthesis of BTK Inhibitor BIIB068,Organic Process Research & Development

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Process Development and Large-Scale Synthesis of BTK Inhibitor BIIB068
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2020-04-21 , DOI: 10.1021/acs.oprd.0c00087
Chaomin Li ₁ , Lloyd Franklin ₁ , Robbie Chen ₁ , Tamera Mack ₁ , Michael Humora ₁ , Bin Ma ₂ , Brian T. Hopkins ₂ , John Guzowski ₁ , Fengmei Zheng ₃ , Michael MacPhee ₃ , Yiqing Lin ₃ , Steven Ferguson ₁ , Daniel Patience ₁ , George A. Moniz ₄ , William F. Kiesman ₁ , Erin M. O’Brien ₁

Affiliation

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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