Radiosynthesis of a Bruton's tyrosine kinase inhibitor, [11C]Tolebrutinib, via palladium‐NiXantphos‐mediated carbonylation

• Published in: Journal of labelled compounds & radiopharmaceuticals Vol. 63; no. 11; pp. 482 - 487
• Main Authors: Dahl, Kenneth, Turner, Timothy, Vasdev, Neil
• Format: Journal Article
• Language: English
• Published: HOBOKEN Wiley 01.09.2020; Wiley Subscription Services, Inc
• Subjects: Acrylamide; Agammaglobulinaemia Tyrosine Kinase - antagonists & inhibitors; aminocarbonylation; Biochemical Research Methods; Biochemistry & Molecular Biology; Bruton's tyrosine kinase; BTK; Carbon monoxide; Carbon Radioisotopes - chemistry; Carbonyls; carbon‐11; Chemistry; Chemistry Techniques, Synthetic; Chemistry, Analytical; Chemistry, Medicinal; Emission analysis; Enzyme inhibitors; Kinases; Life Sciences & Biomedicine; Medical imaging; Multiple sclerosis; Palladium; Palladium - chemistry; PET; Pharmacology & Pharmacy; Physical Sciences; Positron emission; Positron emission tomography; Positron-Emission Tomography - methods; Protein Kinase Inhibitors - chemical synthesis; Protein Kinase Inhibitors - chemistry; Radiochemistry; Radiopharmaceuticals - chemical synthesis; Radiopharmaceuticals - chemistry; Science & Technology; Signal transduction; Synthesis; Target recognition; Tomography; Tyrosine; Tyrosine kinase inhibitors; ACID; C-11-CARBONYLATION; MONOXIDE; BTK; carbon-11; PET; radiochemistry; LABELING CHEMISTRY; aminocarbonylation

Bruton's tyrosine kinase (BTK) is a key component in the B‐cell receptor signaling pathway and is consequently a target for in vivo imaging of B‐cell malignancies as well as in multiple sclerosis (MS) with positron emission tomography (PET). A recent Phase 2b study with Sanofi's BTK inhibi...