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Synthesis of C-14 labeled Rac-(3R,2S )-Glycopyrronium Bromide
Journal of Labelled Compounds and Radiopharmaceuticals ( IF 0.9 ) Pub Date : 2020-07-01 , DOI: 10.1002/jlcr.3864
Jonas Bergare 1 , Neil Nixon 2 , Jeffery Newsome 2 , Linda Thunberg 1 , Charles S Elmore 1
Affiliation  

In an effort to better understand the 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 Cu14 CN. 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 [14 C]-1.

中文翻译:


C-14标记的Rac-(3R,2S)-格隆溴铵的合成



为了更好地了解格隆溴铵 (1)(一种毒蕈碱乙酰胆碱受体拮抗剂)的 DMPK 特性,需要使用 C-14 标记的同位素体。该化合物通过五个合成步骤制备而成,Cu14 CN 的总放射化学产率为 5%。在合成过程中,苯基乙醛酸的意外脱羧导致大量放射性标记化合物的损失。利用手性色谱分离并递送正确的对映体对作为[14C]-1。
更新日期:2020-07-01
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