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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.

中文翻译:

BTK抑制剂BIIB068的工艺开发和大规模合成

讨论了导致多千克生产BIIB068半己二酸酯的化学工艺开发工作。工艺的优化导致(1)从工艺中去除过渡金属;(2)精简的工艺具有显着提高的总收率;(3)适当的杂质控制(包括潜在的诱变杂质),从而可以提供用于毒理学研究的优质材料和临床试验。
更新日期:2020-06-19
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