Synthesis of the derivatives of 6-amino-uracil labelled with C-14

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F16%3A00471547" target="_blank" >RIV/61388963:_____/16:00471547 - isvavai.cz</a>

Výsledek na webu

<a href="http://dx.doi.org/10.1002/jlcr.3405" target="_blank" >http://dx.doi.org/10.1002/jlcr.3405</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1002/jlcr.3405" target="_blank" >10.1002/jlcr.3405</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Synthesis of the derivatives of 6-amino-uracil labelled with C-14

Popis výsledku v původním jazyce

The radioactively labelled 6-amino-5-nitroso-uracil (1) and 5-acetyl-6-amino-1,3-dimethyl-uracil (2) were required for metabolic studies to assess their suitability as drug candidates. A common precursor for both compounds was [cyano-C-14] cyanoacetic acid (6), readily prepared from potassium [C-14]cyanide. ACS reagents, namely, diethyl ether, acetic acid and acetic anhydride, had to be rigorously repurified to achieve a successful synthesis of C-14-labelled compounds on a tenth-of-a-milligramme scale. 6-Amino-5-nitroso-[6-C-14] uracil (1-C-14) (0.55 mCi) was prepared with radiochemical purity>98% and specific activity (SA) = 55.6 mCi/mmol. 5-Acetyl-6-amino-1,3-dimethyl-[6-C-14] uracil (2-C-14) (8 mCi) was prepared with radiochemical purity>97% and SA = 55.6 mCi/mmol. It has been shown that a SA assay can be made from standard C-13 NMR spectra, thus avoiding the need to perform lengthier inverse-gated C-13 NMR experiments.

Název v anglickém jazyce

Synthesis of the derivatives of 6-amino-uracil labelled with C-14

Popis výsledku anglicky

The radioactively labelled 6-amino-5-nitroso-uracil (1) and 5-acetyl-6-amino-1,3-dimethyl-uracil (2) were required for metabolic studies to assess their suitability as drug candidates. A common precursor for both compounds was [cyano-C-14] cyanoacetic acid (6), readily prepared from potassium [C-14]cyanide. ACS reagents, namely, diethyl ether, acetic acid and acetic anhydride, had to be rigorously repurified to achieve a successful synthesis of C-14-labelled compounds on a tenth-of-a-milligramme scale. 6-Amino-5-nitroso-[6-C-14] uracil (1-C-14) (0.55 mCi) was prepared with radiochemical purity>98% and specific activity (SA) = 55.6 mCi/mmol. 5-Acetyl-6-amino-1,3-dimethyl-[6-C-14] uracil (2-C-14) (8 mCi) was prepared with radiochemical purity>97% and SA = 55.6 mCi/mmol. It has been shown that a SA assay can be made from standard C-13 NMR spectra, thus avoiding the need to perform lengthier inverse-gated C-13 NMR experiments.

Druh

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

CEP obor

CC - Organická chemie

OECD FORD obor

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Projekt

<a href="/cs/project/LG13002" target="_blank" >LG13002: Členství ve Vědecké radě Středoevropské divize International Isotope Society.</a><br>

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2016

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

—

Svazek periodika

59

Číslo periodika v rámci svazku

14

Stát vydavatele periodika

GB - Spojené království Velké Británie a Severního Irska

Počet stran výsledku

4

Strana od-do

615-618

Kód UT WoS článku

000392837700005

EID výsledku v databázi Scopus

2-s2.0-84971442603