The preparation of the 61-specific ligand 7-benzylidenenaltrexone (BNTX), labeled with tritium at high specific activity (14.4 Ciimmol) was prepared in 33% yield and >98% purity by the aldol condensation of high specific activity [15,1 6-3H]naltrexone with benzaldehyde at high dilution.
Synthesis of high specific activity [15,16-3H2]buprenorphine
✍ Scribed by Ferenc Ötvös; Sándor Hosztafi; Csaba Simon; Géza Tóth
- Publisher
- John Wiley and Sons
- Year
- 1995
- Tongue
- French
- Weight
- 225 KB
- Volume
- 36
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Tritium labelling of buprenorphine, a mixed agonist-antagonist opioid ligand, was performed with a specific activity of 2.35 TBq/mmol (63.6 Ci/mrnol) starting with 15,16-didehydrobuprenorphine. Labels at positions 15 and 16 of the morphine skeleton proved to be sufficiently stable under strong acidic or basic conditions.
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## Abstract Mercury(II) oxide oxidation of naltrexone (1a) and naloxone (1b) gave 15,16‐didehydronaltrexone (4a) and 15,16 didehydronaloxone (4b). Subsequent reduction of 4a with tritium gas afforded naltrexone‐15,16‐^3^H~2~ having a‐specific activity of 15.3 Ci/mmole. Subsequent equilibration of 4
## Abstract The title compounds, each of high isotopic purity, were synthesized as internal standards for the mass spectral quantitation of estradiol and estrone. The [^2^H~3~] estradiol **3** was obtained from estrone (**1**) by alkaline H/^2^H exchange of the C‐16 protons and LiAl^2^LH~4~ reducti
The title compound has been prepared by two different approaches. The first involved a five-stage "hot" synthesis.where the tritiation step was selective debromination of a cyclic Fbromo-a-&unsaturated ketone. double bond was protected by formal aromatisation. this intermediate was determined by pro