Buscopan labeled with carbon‐14 and deuterium |
| |
| Authors: | Bachir Latli Michael Stiasni Matt Hrapchak Zhibin Li Nelu Grinberg Heewon Lee Carl A. Busacca Chris H. Senanayake |
| |
| Affiliation: | 1. Chemical Development, Boehringer Ingelheim Pharmaceuticals, Inc, Ridgefield, CT, USA;2. Boehringer Ingelheim GmbH & Co KG, Ingelheim am Rhein, Germany |
| |
| Abstract: | Hyosine butyl bromide, the active ingredient in Buscopan, is an anticholinergic and antimuscarinic drug used to treat pain and discomfort caused by abdominal cramps. A straightforward synthesis of carbon‐14– and deuterium‐labeled Buscopan was developed using scopolamine, n‐butyl‐1‐14C bromide, and n‐butyl‐2H9 bromide, respectively. In a second carbon‐14 synthesis, the radioactive carbon was incorporated in the tropic acid moiety to follow its metabolism. Herein, we describe the detailed preparations of carbon‐14– and deuterium‐labeled Buscopan. |
| |
| Keywords: | Buscopan carbon‐14 deuterium hyoscine butyl bromide radiosynthesis tropic acid |
|
|
