Buscopan labeled with carbon‐14 and deuterium. (17th October 2016)

• Record Type: Journal Article
• Authors: Latli, Bachir; Stiasni, Michael; Hrapchak, Matt; Li, Zhibin; Grinberg, Nelu; Lee, Heewon; Busacca, Carl A.; Senanayake, Chris H.
• Is Part Of: Journal of labelled compounds & radiopharmaceuticals. Volume 59:Number 13(2016)
• Page Start: 557
• Page End: 564
• Publication Date: 2016-10-17
• Subjects: Buscopan -- carbon‐14 -- deuterium -- hyoscine butyl bromide -- radiosynthesis -- tropic acid; Tracers (Chemistry) -- Periodicals; Radiopharmaceuticals -- Periodicals; 615.8424
• DOI: 10.1002/jlcr.3463
• Languages: English
• ISSNs: 0362-4803

Abstract

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‐ 14 C bromide, and n ‐butyl‐ 2 H 9 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. Abstract : A straightforward synthesis of carbon‐14 and deuterium‐labeled Buscopan was developed using scopolamine, n ‐butyl‐1‐ 14 C bromide, and n ‐butyl‐ 2 H 9 bromide, respectively. In a second carbon‐14 synthesis, the radioactive carbon was incorporated in the tropic acid moiety. The detailed preparations of carbon‐14 and deuterium‐labeled Buscopan are reported.