Towards stereoselective radiosynthesis of ?-[11C]methylsubtituted aromatic ?-amino acids ? a challenge of creation of quaternary asymmetric centre in a very short time.

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216275%3A25310%2F07%3A00006287" target="_blank" >RIV/00216275:25310/07:00006287 - isvavai.cz</a>

Výsledek na webu

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DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

Towards stereoselective radiosynthesis of ?-[11C]methylsubtituted aromatic ?-amino acids ? a challenge of creation of quaternary asymmetric centre in a very short time.

Popis výsledku v původním jazyce

In positron emission tomography (PET) a-methyl amino acids have two potential applications: As analogues of neutransmitter precursors for the study of neurodegenerative diseases, and as non-metabolised analogues of proteinogenic amino acids for the studyof amino acid uptake into normal and cancer cells. Clinical applications of such amino acids are strongly limited due to their poor availability. We carried out [11C]methylation of metalocomplex synthons derived from protected DOPA or tyrosine. For [11C]methylation, sodium hydroxide (5mg of fine dry powder) was sealed in a vial, which was flushed with dry nitrogen before addition of a solution of the complex (10 mg) and 11CH3I in 1,3-dimethylimidazolidin-2-one (300 ml). After 10 min at 258C, a 9% radiochemical yield (decay-corrected) of a mixture of the diastereomeric a-[11C]methylDOPA complexes or a 7% radiochemical yield of a mixture of the diastereomeric a-[11C]methyltyrosine complexes was achieved. Individual diastereomers were suc

Název v anglickém jazyce

Towards stereoselective radiosynthesis of ?-[11C]methylsubtituted aromatic ?-amino acids ? a challenge of creation of quaternary asymmetric centre in a very short time.

Popis výsledku anglicky

In positron emission tomography (PET) a-methyl amino acids have two potential applications: As analogues of neutransmitter precursors for the study of neurodegenerative diseases, and as non-metabolised analogues of proteinogenic amino acids for the studyof amino acid uptake into normal and cancer cells. Clinical applications of such amino acids are strongly limited due to their poor availability. We carried out [11C]methylation of metalocomplex synthons derived from protected DOPA or tyrosine. For [11C]methylation, sodium hydroxide (5mg of fine dry powder) was sealed in a vial, which was flushed with dry nitrogen before addition of a solution of the complex (10 mg) and 11CH3I in 1,3-dimethylimidazolidin-2-one (300 ml). After 10 min at 258C, a 9% radiochemical yield (decay-corrected) of a mixture of the diastereomeric a-[11C]methylDOPA complexes or a 7% radiochemical yield of a mixture of the diastereomeric a-[11C]methyltyrosine complexes was achieved. Individual diastereomers were suc

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

CA - Anorganická chemie

OECD FORD obor

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Projekt

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Návaznosti

Z - Vyzkumny zamer (s odkazem do CEZ)

Rok uplatnění

2007

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Journal of Labelled Compounds and Radiopharmaceuticals

ISSN

0362-4803

e-ISSN

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Svazek periodika

50

Číslo periodika v rámci svazku

2

Stát vydavatele periodika

GB - Spojené království Velké Británie a Severního Irska

Počet stran výsledku

5

Strana od-do

370-374

Kód UT WoS článku

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EID výsledku v databázi Scopus

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