Buscopan labeled with carbon-14 and deuterium

被引：5

作者：

Latli, Bachir ^{[1
]}

Stiasni, Michael ^{[2
]}

Hrapchak, Matt ^{[1
]}

Li, Zhibin ^{[1
]}

Grinberg, Nelu ^{[1
]}

Lee, Heewon ^{[1
]}

Busacca, Carl A. ^{[1
]}

Senanayake, Chris H. ^{[1
]}

机构：

[1] Boehringer Ingelheim Pharmaceut Inc, Chem Dev, 900 Ridgebury Rd,POB 368, Ridgefield, CT 06877 USA

[2] Boehringer Ingelheim GmbH & Co KG, Binger Str 173, D-55216 Ingelheim, Germany

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2016年 / 59卷 / 13期

关键词：

Buscopan; carbon-14; deuterium; hyoscine butyl bromide; radiosynthesis; tropic acid; TROPIC ACID; TROPANE ALKALOIDS; HYOSCINE BUTYLBROMIDE; KINETIC RESOLUTION; DERIVATIVES; ATROPINE; STEREOCHEMISTRY; BIOSYNTHESIS;

D O I：

10.1002/jlcr.3463

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

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-C-14 bromide, and n-butyl-H-2(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.

引用

页码：557 / 564

页数：8

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