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. 2008 Oct;66(10):1414-8.
doi: 10.1016/j.apradiso.2008.02.076. Epub 2008 Mar 10.

Improved and semi-automated GMP-compliant radiosynthesis of [11C]docetaxel

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Improved and semi-automated GMP-compliant radiosynthesis of [11C]docetaxel

E W van Tilburg et al. Appl Radiat Isot. 2008 Oct.

Abstract

[(11)C]Docetaxel (Taxotere) has been synthesized via an improved synthesis route, which involves a more efficient intermediate removal of the excess 1,2,2,2-tetrachloroethyl chloroformate. Furthermore, the purification and formulation into a human applicable solution of [(11)C]docetaxel was developed. 1,2,2,2-Tetrachloroethyl chloroformate is used for the synthesis of the intermediate [(11)C]tert-butyl-1,2,2,2-tetrachloroethyl carbonate that in the final reaction step reacts with the precursor, the primary amine of docetaxel, yielding [(11)C]docetaxel. The purified and isolated product was obtained in 10+/-2% overall decay-corrected radiochemical yield. The total synthesis time was 67 min and the specific activity was 9-17 GBq/micromol (N=7).

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