Synthesis of a11C-labelled taxane derivative by [1-11C]acetylation
| Autor: | J. Zessin, P. Mäding, F. Wüst, U. Pleiß, F. Füchtner |
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| Rok vydání: | 2006 |
| Předmět: |
Taxane
Chemistry Organic Chemistry Extraction (chemistry) Radiochemistry Total synthesis Biochemistry High-performance liquid chromatography Chemical synthesis Analytical Chemistry chemistry.chemical_compound Acetylation Acetyl chloride Yield (chemistry) Drug Discovery Organic chemistry Radiology Nuclear Medicine and imaging Spectroscopy |
| Zdroj: | Journal of Labelled Compounds and Radiopharmaceuticals. 49:357-365 |
| ISSN: | 1099-1344 0362-4803 |
| DOI: | 10.1002/jlcr.1059 |
| Popis: | The 11C-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 [11C]1 was synthesized by reacting [1-11C]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 [11C]1, its solid-phase extraction, formulation and sterile filtration, the decay-corrected radiochemical yield of [11C]1 was in the range between 12 and 23% (related to [11C]CO2; n=10). The total synthesis time was about 54 min after EOB. The radiochemical purity of [11C]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 [11C]CO2. Copyright © 2006 John Wiley & Sons, Ltd. |
| Databáze: | OpenAIRE |
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