Large-scale synthesis of a Notum inhibitor employing a modified Sakai reaction as the key step

WuXi AppTec scientists recently contributed to a research article in the Royal Society of Chemistry describing the large-scale synthesis of a potent and selective inhibitor of Notum carboxylesterase (an enzyme that suppresses Wnt signaling pathways). By employing a modified Sakai reaction as the key step, a one-pot synthesis of this Notum inhibitor was developed, enabling the delivery of multi-gram quantities for use in preclinical toxicology studies.
https://pubmed.ncbi.nlm.nih.gov/36275171/

Large-scale synthesis of a Notum inhibitor employing a modified Sakai reaction as the key step
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