Improved method for preparing Ni(II) complex of (S)-tyrosine Schiff base and its use in the automated synthesis of O-(2′-[ 18 F]fluoroethyl)- l -tyrosine using solid-phase extraction purification

We found that acetonitrile acted as a reactant under the conventional reaction conditions for aliphatic nucleophilic 18 Ffluorination in acetonitrile to provide the N-alkyl 3-aminobut-2enenitrile as one of the side products. Dimerization of acetonitrile promoted by a complex of K 2 CO 3 and K222 provided 3-aminobut-2-enenitrile, which acted as nucleophile to provide N-alkyl amino derivatives. Based on the finding, avoiding acetonitrile in the drying of [ 18 F]fluoride as well as 18 Flabeling enabled the preparation of 18 F-labeled compounds containing only a small amount of the corresponding alcohol. Finally, we used an automated synthesizer to achieve an efficient phase-tag-assisted synthesis of 18 F-labeled stilbene derivative as a 18 F-labeled amyloid-β ligand.

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N‐Alkyl 3‐aminobut‐2‐enenitrile as a Non‐radioactive Side Product in Nucleophilic ¹⁸F‐Fluorination

Song

Tago

Tatsuta

et al. 2021

ChemistrySelect

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A fully automated azeotropic drying free synthesis of O-(2-[18F]fluoroethyl)- -tyrosine ([18F]FET) using tetrabutylammonium tosylate

Orlovskaya

Федорова

Nadporojskii

et al. 2019

Applied Radiation and Isotopes

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Use of capillary electrophoresis for the determination of impurities in preparations of fluorine-18 labelled PET radiopharmaceuticals

Antuganov

Antuganova

Зыкова

et al. 2019

Journal of Pharmaceutical and Biomedical Analysis

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Improved method for preparing Ni(II) complex of (S)-tyrosine Schiff base and its use in the automated synthesis of O-(2′-[ 18 F]fluoroethyl)- l -tyrosine using solid-phase extraction purification

Cited by 4 publications

References 25 publications

N‐Alkyl 3‐aminobut‐2‐enenitrile as a Non‐radioactive Side Product in Nucleophilic ¹⁸F‐Fluorination

N‐Alkyl 3‐aminobut‐2‐enenitrile as a Non‐radioactive Side Product in Nucleophilic ¹⁸F‐Fluorination

A fully automated azeotropic drying free synthesis of O-(2-[18F]fluoroethyl)- -tyrosine ([18F]FET) using tetrabutylammonium tosylate

Use of capillary electrophoresis for the determination of impurities in preparations of fluorine-18 labelled PET radiopharmaceuticals

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Improved method for preparing Ni(II) complex of (S)-tyrosine Schiff base and its use in the automated synthesis of O-(2′-[ 18 F]fluoroethyl)- l -tyrosine using solid-phase extraction purification

Cited by 4 publications

References 25 publications

N‐Alkyl 3‐aminobut‐2‐enenitrile as a Non‐radioactive Side Product in Nucleophilic 18F‐Fluorination

N‐Alkyl 3‐aminobut‐2‐enenitrile as a Non‐radioactive Side Product in Nucleophilic 18F‐Fluorination

A fully automated azeotropic drying free synthesis of O-(2-[18F]fluoroethyl)- -tyrosine ([18F]FET) using tetrabutylammonium tosylate

Use of capillary electrophoresis for the determination of impurities in preparations of fluorine-18 labelled PET radiopharmaceuticals

Contact Info

Product

Resources

About

N‐Alkyl 3‐aminobut‐2‐enenitrile as a Non‐radioactive Side Product in Nucleophilic ¹⁸F‐Fluorination

N‐Alkyl 3‐aminobut‐2‐enenitrile as a Non‐radioactive Side Product in Nucleophilic ¹⁸F‐Fluorination