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- Title
Synthesis of C‐14 labeled Rac‐(3R,2S)‐glycopyrronium bromide.
- Authors
Bergare, Jonas; Nixon, Neil; Newsome, Jeffery; Thunberg, Linda; Elmore, Charles S.
- Abstract
In an effort to better understand the drug metabolism and pharmacokinetics (DMPK) properties of glycopyrronium bromide (1), a muscarinic acetylcholine receptor antagonist, a C‐14 labeled isotopologue was required. The compound was prepared in five synthetic steps and 5% overall radiochemical yield from Cu14CN. During the synthesis, an unexpected decarboxylation of phenylglyoxylate resulted in the loss of much of the radiolabeled compound. Chiral chromatography was utilized to isolate and deliver the proper pair of enantiomers as [14C]‐1.
- Subjects
GLYCOPYRROLATE; MUSCARINIC acetylcholine receptors; DRUG metabolism; CHOLINERGIC receptors; PHARMACOKINETICS; BROMIDES
- Publication
Journal of Labelled Compounds & Radiopharmaceuticals, 2020, Vol 63, Issue 10, p456
- ISSN
0362-4803
- Publication type
Academic Journal
- DOI
10.1002/jlcr.3864