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Synthesis of a 11C-labelled taxane derivative by [1-11C]acetylation

✍ Scribed by P. Mäding; J. Zessin; U. Pleiß; F. Füchtner; F. Wüst

Publisher
John Wiley and Sons
Year
2006
Tongue
French
Weight
173 KB
Volume
49
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

The ^11^C‐labelling of the taxane derivative BAY 59‐8862 (1), a potent anticancer drug, was carried out as a module‐assisted automated multi‐step synthesis procedure. The radiotracer [^11^C]1 was synthesized by reacting [1‐^11^C]acetyl chloride (6) with the lithium salt of the secondary hydroxy group of precursor 3 followed by deprotection. After HPLC purification of the final product [^11^C]1, its solid‐phase extraction, formulation and sterile filtration, the decay‐corrected radiochemical yield of [^11^C]1 was in the range between 12 and 23% (related to [^11^C]CO~2~; n=10). The total synthesis time was about 54 min after EOB. The radiochemical purity of [^11^C]1 was greater than 96% and the chemical purity exceeded 80%. The specific radioactivity was 16.8±4.7 GBq/µmol (n=10) at EOS starting from 80 GBq of [^11^C]CO~2~. Copyright © 2006 John Wiley & Sons, Ltd.

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