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Issue 6, 2004

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.

Article information


Submitted
26 May 2004
Accepted
10 Sep 2004
First published
28 Sep 2004

Lab Chip, 2004,4, 523-525
Article type
Communication

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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