Journal
ORGANIC PROCESS RESEARCH & DEVELOPMENT
Volume 23, Issue 6, Pages 1143-1151Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.oprd.8b00398
Keywords
atropisomer; Bruton's tyrosine kinase; chiral axis; optimization; high-throughput experiments
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The development of a telescoped process for the API step in the route to a reversible inhibitor of BTK is reported. Although a robust and effective reaction and crystallization was previously implemented, concerns around the storage and stability of the penultimate material led to investigating a telescoped process. Utilizing design of experiments (DoE) to understand impacts to the API reaction and high-throughput extractions (HTEx) to optimize the workup, a process was rapidly developed to achieve the same quality API with an overall 13% improvement to yield and 41% improvement in the process mass intensity (PMI).
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