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Radiosynthesis of [11C]docetaxel

✍ Scribed by E. W. van Tilburg; E. J. F. Franssen; J. J. M. van der Hoeven; M. van der Meij; D. Elshove; A. A. Lammertsma; A. D. Windhorst

Publisher
John Wiley and Sons
Year
2004
Tongue
French
Weight
166 KB
Volume
47
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Docetaxel (Taxotere®) is an accepted chemotherapeutic agent for the treatment of breast cancer and non‐small cell lung cancers. A potential means of predicting response is measuring tumor uptake of [^11^C]docetaxel using Positron Emission Tomography (PET). The synthetic approach to introduce the ^11^C isotope in the 2‐benzoyl moiety of docetaxel unfortunately was unsuccessful. The radiosynthesis of [^11^C]docetaxel (6b, Scheme 1), with the ^11^C isotope in the BOC moiety, was however, successful using a second synthetic approach. It started with the reaction of [^11^C]tert‐butanol with 1,2,2,2‐tetrachloroethyl chloroformate to give [^11^C]tert‐butyl‐l,2,2,2‐tetrachloroethyl carbonate in a good overall yield (62±9%). In the final step, the [^11^C]tert‐butoxycarbonylation of the free amine of docetaxel gave [^11^C]docetaxel 6b in a satisfactory decay corrected yield of 10±1% (from [^11^C]CO~2~). Copyright © 2004 John Wiley & Sons, Ltd.

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