3H-Sch 47949, racemic 3H-Sch 48461, was prepared at a specific activity of 40 mCi/mmole by Pt catalysed exchange with tritiated water. 3H-Sch 48461 was prepared at a specific activity of 64.6 Ci/mmole by a Pd/C catalysed reduction of an olefinic intermediate. 14C-Sch 48461 was prepared in 8 steps fr
3H- and 14C-labelling of the aromatase inhibitor ZK 138723
β Scribed by J. Gay; P. Strehlke
- Publisher
- John Wiley and Sons
- Year
- 1996
- Tongue
- French
- Weight
- 239 KB
- Volume
- 38
- Category
- Article
- ISSN
- 0022-2135
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β¦ Synopsis
Synthesis of the 3H-and 14C-labelled aromatase inhibitor ZK138723 is described+. The 3H-label was obtained by dehalogenation of a 4,5-diiodoimidazole derivative with tritium gas, yielding 30.8 mCi with a specific activity of 33.4 Cilmmol. Bromine replacement in the thiophene a-position by [14C]cyanide afforded 25.9 mCi of the 14C-labelled material with a specific activity of 55.6 mCi/mmol.
π SIMILAR VOLUMES
\({ }^{3} \mathrm{H}\) and \({ }^{14} \mathrm{C}\)-Sch 27899 have been prepared by fermentation using the Micromonospora carbonacea organism. In the case of \({ }^{3} \mathrm{H}\)-Sch 27899 , the label was incorporated by a single addition of \(100 \mathrm{mCi}\) of \(70 \mathrm{Ci} / \mathrm{mmole}