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The Effect of Reaction Media and Phase Transfer Catalyst on the Fluorination Yield and Enantiomeric Purity in Asymmetric Synthesis of O-(2 '-[F-18]fluoroethyl)-L-Tyrosine ([F-18]FET). / Krasikova, Raisa; Orlovskaya, Victoria; Stepanova, Maria; Fedorova, Olga.

в: Current Organic Chemistry, Том 17, № 19, 2013.

Результаты исследований: Научные публикации в периодических изданияхстатья

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Krasikova, Raisa ; Orlovskaya, Victoria ; Stepanova, Maria ; Fedorova, Olga. / The Effect of Reaction Media and Phase Transfer Catalyst on the Fluorination Yield and Enantiomeric Purity in Asymmetric Synthesis of O-(2 '-[F-18]fluoroethyl)-L-Tyrosine ([F-18]FET). в: Current Organic Chemistry. 2013 ; Том 17, № 19.

BibTeX

@article{262531ecaf304a1c9be4bb6e785f0906,
title = "The Effect of Reaction Media and Phase Transfer Catalyst on the Fluorination Yield and Enantiomeric Purity in Asymmetric Synthesis of O-(2 '-[F-18]fluoroethyl)-L-Tyrosine ([F-18]FET)",
abstract = "Due to favourable in-vivo characteristics, the long half-life of F-18 (110 min) allowing for remote-site delivery and its high specificity, O-(2'-[F-18]fluoroethyl)-L-tyrosine ([F-18]FET) has gained increased importance for molecular imaging of cerebral tumors. Consequently, the development of simple and efficient production strategies for FET could be an important step to further improve the cost-effective availability of FET in the clinical environment. An earlier developed labeling approach using a chiral Ni-II complex of an alkylated (S)-tyrosine Schiff base, Ni-(S)-BPB-(S)-Tyr-OCH2CH2OTs (II) as a synthesis precursor provided a good means of preparing FET in high enantiomeric purity of 94-97%, but in moderate RCY. The aim of this study was to improve the F-18-fluorination efficiency of (II) by varying fluorinations conditions: reaction media (non protic and protic solvents), PTC/base system and temperature. A very high F-18-fluoride incorporation rate into (II) was achieved in kryptofix-mediated fluorina",
author = "Raisa Krasikova and Victoria Orlovskaya and Maria Stepanova and Olga Fedorova",
year = "2013",
language = "English",
volume = "17",
journal = "Current Organic Chemistry",
issn = "1385-2728",
publisher = "Bentham Science Publishers B.V.",
number = "19",

}

RIS

TY - JOUR

T1 - The Effect of Reaction Media and Phase Transfer Catalyst on the Fluorination Yield and Enantiomeric Purity in Asymmetric Synthesis of O-(2 '-[F-18]fluoroethyl)-L-Tyrosine ([F-18]FET)

AU - Krasikova, Raisa

AU - Orlovskaya, Victoria

AU - Stepanova, Maria

AU - Fedorova, Olga

PY - 2013

Y1 - 2013

N2 - Due to favourable in-vivo characteristics, the long half-life of F-18 (110 min) allowing for remote-site delivery and its high specificity, O-(2'-[F-18]fluoroethyl)-L-tyrosine ([F-18]FET) has gained increased importance for molecular imaging of cerebral tumors. Consequently, the development of simple and efficient production strategies for FET could be an important step to further improve the cost-effective availability of FET in the clinical environment. An earlier developed labeling approach using a chiral Ni-II complex of an alkylated (S)-tyrosine Schiff base, Ni-(S)-BPB-(S)-Tyr-OCH2CH2OTs (II) as a synthesis precursor provided a good means of preparing FET in high enantiomeric purity of 94-97%, but in moderate RCY. The aim of this study was to improve the F-18-fluorination efficiency of (II) by varying fluorinations conditions: reaction media (non protic and protic solvents), PTC/base system and temperature. A very high F-18-fluoride incorporation rate into (II) was achieved in kryptofix-mediated fluorina

AB - Due to favourable in-vivo characteristics, the long half-life of F-18 (110 min) allowing for remote-site delivery and its high specificity, O-(2'-[F-18]fluoroethyl)-L-tyrosine ([F-18]FET) has gained increased importance for molecular imaging of cerebral tumors. Consequently, the development of simple and efficient production strategies for FET could be an important step to further improve the cost-effective availability of FET in the clinical environment. An earlier developed labeling approach using a chiral Ni-II complex of an alkylated (S)-tyrosine Schiff base, Ni-(S)-BPB-(S)-Tyr-OCH2CH2OTs (II) as a synthesis precursor provided a good means of preparing FET in high enantiomeric purity of 94-97%, but in moderate RCY. The aim of this study was to improve the F-18-fluorination efficiency of (II) by varying fluorinations conditions: reaction media (non protic and protic solvents), PTC/base system and temperature. A very high F-18-fluoride incorporation rate into (II) was achieved in kryptofix-mediated fluorina

M3 - Article

VL - 17

JO - Current Organic Chemistry

JF - Current Organic Chemistry

SN - 1385-2728

IS - 19

ER -

ID: 7544894