Remote controlled production of [2‐<sup>11</sup>C] isopropyl iodide

SummaryThe novel CCK-A agonist, (S)-3-(3-f1-[(isopropylphenylcarbamoyl)methyl]-2,4-dioxo-5-phenyl-2,3,4,5-tetrahydro-1H-benzo [b][1,4]diazepin-3-ylgureido)benzoic acid, GI181771 ((S)-1) has been isotopically labelled with carbon-11 at its urea site using [ 11 C]phosgene in a one-pot two-step process, via the intermediate preparation of an specific radioactivities ranging from 500 to 1500 mCi/mmol (18.5-55.5 GBq/mmol). The radiotracer preparation was a clear and colourless solution and its pH was between 5 and 7. As demonstrated by HPLC analysis, the radiolabelled product was found to be >99% chemically and radiochemically pure and the preparation was shown to be free of non-radioactive precursors (starting amines) and radiochemically stable for at least 60 min. Finally, enantiomeric purity was found to be >99%

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Radiosynthesis of carbon‐11‐labelled GI181771, a new selective CCK‐A agonist

Dollé

Martarello

Bramoullé

et al. 2005

Labelled Comp Radiopharmac

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Synthesis of [isopropyl-11C]nimodipine for in vivo studies of dihydropyridine binding in man using positron emission tomography

Stone‐Elander¹,

Roland²,

Schwenner

et al. 1991

International Journal of Radiation Applications and Instrumenta

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Rapid synthesis of aliphatic amides by reaction of carboxylic acids, Grignard reagent and amines: application to the preparation of [11C]amides

Aubert¹,

Huard‐Perrio²,

Lasne³

1997

J. Chem. Soc., Perkin Trans. 1

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Remote controlled production of [2‐¹¹C] isopropyl iodide

Cited by 3 publications

References 3 publications

Radiosynthesis of carbon‐11‐labelled GI181771, a new selective CCK‐A agonist

Radiosynthesis of carbon‐11‐labelled GI181771, a new selective CCK‐A agonist

Synthesis of [isopropyl-11C]nimodipine for in vivo studies of dihydropyridine binding in man using positron emission tomography

Rapid synthesis of aliphatic amides by reaction of carboxylic acids, Grignard reagent and amines: application to the preparation of [11C]amides

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Remote controlled production of [2‐11C] isopropyl iodide

Cited by 3 publications

References 3 publications

Radiosynthesis of carbon‐11‐labelled GI181771, a new selective CCK‐A agonist

Radiosynthesis of carbon‐11‐labelled GI181771, a new selective CCK‐A agonist

Synthesis of [isopropyl-11C]nimodipine for in vivo studies of dihydropyridine binding in man using positron emission tomography

Rapid synthesis of aliphatic amides by reaction of carboxylic acids, Grignard reagent and amines: application to the preparation of [11C]amides

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Remote controlled production of [2‐¹¹C] isopropyl iodide