Результаты исследований: Научные публикации в периодических изданиях › статья
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 изданиях › статья
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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