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Synthesis of a 11 C‐labelled taxane derivative by [1‐ 11 C]acetylation
Author(s) -
Mäding P.,
Zessin J.,
Pleiß U.,
Füchtner F.,
Wüst F.
Publication year - 2006
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.1059
Subject(s) - chemistry , yield (engineering) , radiochemistry , derivative (finance) , extraction (chemistry) , specific activity , chloride , chemical synthesis , labelling , nuclear chemistry , high performance liquid chromatography , chromatography , organic chemistry , in vitro , biochemistry , materials science , economics , financial economics , metallurgy , enzyme
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.