Stereoselectivní radiosyntéza alfa-[C-11]methylsubstituovaných aromatických alfa-amino acids ? stimul k syntéze kvarterního asymetrického centra ve velmi krátké době

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60077344%3A_____%2F07%3A00094858" target="_blank" >RIV/60077344:_____/07:00094858 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/60076658:12640/07:00008324

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 alpha-[C-11]methylsubstituted aromatic alpha-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) alpha-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 study of 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 [C-11]methylation of metalocomplex synthons derived from protected DOPA or tyrosine. After 10min at 25 ?C, a 9% radiochemical yield (decay-corrected) of a mixture of the diastereomeric alpha-[C-11]methylDOPA complexes or a 7% radiochemical yield of a mixture of the diastereomeric alpha-[C-11]methyltyrosine complexes was achieved. Optimisation of the procedure including hydrolysis of the complexes (hydrolytic deprotection of enantiomerically pure amino acids) and subsequent purification of the enantiomers of a-[11C]methyID0PA and alpha-[C-11]methyltyrosine is underway.

Název v anglickém jazyce

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

Popis výsledku anglicky

In positron emission tomography (PET) alpha-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 study of 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 [C-11]methylation of metalocomplex synthons derived from protected DOPA or tyrosine. After 10min at 25 ?C, a 9% radiochemical yield (decay-corrected) of a mixture of the diastereomeric alpha-[C-11]methylDOPA complexes or a 7% radiochemical yield of a mixture of the diastereomeric alpha-[C-11]methyltyrosine complexes was achieved. Optimisation of the procedure including hydrolysis of the complexes (hydrolytic deprotection of enantiomerically pure amino acids) and subsequent purification of the enantiomers of a-[11C]methyID0PA and alpha-[C-11]methyltyrosine is underway.

Druh

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

CEP obor

CE - Biochemie

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

5-6

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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