Douglas A. L. Otte, Reed T. Larson, Embarek Alwedi, Travis J. Armiger, Qinghao Chen, Cheol K. Chung, James Corry, Richard Desmond, Patrick S. Fier, Robert D. Franklin, Erik D. Guetschow, Jackson R. Hall, Holst M. Halsey, Clara Hartmanshenn, Lisa Jellett, Nadine Kuhl, François Lévesque, Jonathan P. McMullen, Pratiq A. Patel, Mellie June Paulines, Hong Ren, Vailankanni L. Rodrigues, Serge Ruccolo, Lushi Tan, David A. Thaisrivongs, Kai‐Jiong Xiao,
Nemtabrutinib (MK-1026) is a novel oral Bruton's tyrosine kinase (BTK) inhibitor for treatment of B-cell cancers. An initial synthetic supply route to generate ketone 3 relied on the generation of a highly reactive transient intermediate and the use of n-butyllithium. Cryogenic temperatures (−60 °C) were also required to achieve a modest 61% yield, with one major impurity, resulting from dehalogenation, accounting for the majority of the mass balance. An alternative process was developed to increase ...
Tópico(s): Biochemical and Molecular Research
2024 - American Chemical Society | Organic Process Research & Development