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Issue 6, 2004
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Syntheses of 11C- and 18F-labeled carboxylic esters within a hydrodynamically-driven micro-reactor

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Abstract

Carboxylic esters were successfully labeled with one of two short-lived positron-emitters, carbon-11 or fluorine-18, within a hydrodynamically-driven micro-reactor. The non-radioactive methyl ester 4a was obtained at room temperature; its yield increased with higher substrate concentration and with reduced infusion rate. Radioactive methyl ester 4b was obtained from the reaction of 1 (10 mM) with 2b in 56% decay-corrected radiochemical yield (RCY) at an infusion rate of 10 µL min−1, and when the infusion rate was reduced to 1 µL min−1, the RCY increased to 88%. The synthesis of the non-radioactive fluoroethyl ester 5a from 1 and 3a required heating of the micro-reactor on a heating block at 80 °C (14–17% RCY), whilst the corresponding radioactive 5b from 1 and 3b was obtained in 10% RCY. The radioactive ‘peripheral’ benzodiazepine receptor ligand 7b was obtained from the reaction of acid 6 with labeling agent 2b in 45% RCY at an infusion rate of 10 µL min−1. When the infusion rate was reduced to 1 µL min−1, the RCY increased to 65%. The results exemplify a new methodology for producing radiotracers for imaging with positron emission tomography that has many potential advantages, including a requirement for small quantities of substrates, enhanced reaction, rapid reaction optimisation and easy product purification.

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Publication details

The article was received on 26 May 2004, accepted on 10 Sep 2004 and first published on 28 Sep 2004


Article type: Communication
DOI: 10.1039/B407938H
Lab Chip, 2004,4, 523-525

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    Syntheses of 11C- and 18F-labeled carboxylic esters within a hydrodynamically-driven micro-reactor

    S. Lu, P. Watts, F. T. Chin, J. Hong, J. L. Musachio, E. Briard and V. W. Pike, Lab Chip, 2004, 4, 523
    DOI: 10.1039/B407938H

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