Synthesis and characterization of isotopically labelled drugs

Kaspersen, Frans M.; Vader, J.; Funke, Carel W.; Sperling, Eric M. G.

doi:10.1002/recl.19931120218

Cited by 2 publications

(1 citation statement)

References 12 publications

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“…Similar to [ 3 H]TCDD, decomposition of [13‐ 3 H]mianserin results in the formation of an aryl cation, which reacts with the benzene to form unlabeled 13‐phenylmianserin (Figure 1). 90 [ 14 C]Choline chloride undergoes rapid self‐decomposition when stored as a solid at ambient temperature forming [ 14 C]trimethyl amine and acetaldehyde via carbon–carbon bond cleavage 49,74,75,91,92 . When stored at −80°C, however, [ 14 C]choline chloride is stable showing no decomposition when stored up to 11 months 51,87 .…”

Section: Self‐radiolysis Of T2omentioning

confidence: 99%

Review: Self‐radiolysis of compounds containing tritium and carbon‐14

Wolf

2021

Labelled Comp Radiopharmac

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Energy released from beta emission causes molecules that incorporate tritium (3H) and carbon‐14 (14C) atoms to be less stable than their stable labeled counterparts, thus making radiolabeled compounds prone to self‐radiolysis. This literature review examines the stability of organic compounds incorporating 3H and 14C atoms and discusses stability of the compound with respect to functional groups within the radiolabeled molecules. The goal of this paper is to serve as a reference for the stability of radiolabeled compounds.

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Section: Self‐radiolysis Of T2omentioning

confidence: 99%

Review: Self‐radiolysis of compounds containing tritium and carbon‐14

Wolf

2021

Labelled Comp Radiopharmac

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The syntheses of radiolabelled org 5222 and its main metabolite org 30526

Vader¹,

Kaspersen²,

Sperling³

et al. 1994

Labelled Comp Radiopharmac

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SUMMARYThe syntheses of trans-5-chloro-2,3,3a-l2b-tetrahydro-2-methyl- pyrrole (Org 30526) labelled with 3H are described. 3H-labelled Org 5222 of low specific activity was prepared by a base catalyzed exchange with tritiated water of an amide precursor, 3H-labelled Org 5222 with a high specific activity by a catalytic reductive dehalogenation. 3H-labelled Org 30526 was prepared both by demethylation of 3H-Org 5222 and by catalytic reductive iodination of 11-iodo-Org 30526. l4C-1abelled Org 5222 was synthesized in 6 steps using 14C-sarcosine as starting material. 36C1-labelled Org 5222 was prepared by diazotation reaction in the presence of H3%l.

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Synthesis and characterization of isotopically labelled drugs

Abstract: The article describes approaches for the synthesis and analysis of isotopically (

Cited by 2 publications

References 12 publications

Review: Self‐radiolysis of compounds containing tritium and carbon‐14

Review: Self‐radiolysis of compounds containing tritium and carbon‐14

The syntheses of radiolabelled org 5222 and its main metabolite org 30526

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