## Abstract Carbon‐14 labeled 4‐[4‐[2‐[2‐[bis(4‐chlorophenyl)methoxyethylsulfonyl] [1‐^14^C]ethoxy]phenyl]‐1,1,1‐trifluoro‐2‐butanone was prepared in a six step radioactive synthesis from 2‐bromo[1‐^14^C]acetic acid. The overall radiochemical yield was 2.2%. The specific activity of the final produ
The preparation of carbon-14 labelled 1-[4-(2-diethylamino-ethoxy) phenyl]-1, 2-diphenyl-2-chloroethene (clomiphene) and 1-[4-(2-(N-pyrrolidinyl) ethoxy) phenyl]-2-(4-methoxyphenyl)-2-nitro-2-phenylethene (CI-628, nitromiphene)
✍ Scribed by Peter C. Ruenitz; Jerome R. Bagley
- Publisher
- John Wiley and Sons
- Year
- 1983
- Tongue
- French
- Weight
- 273 KB
- Volume
- 20
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
The preparation of [^14^C] clomiphene and [^14^C] nitromiphene from [methylene‐^14^C] benzyl chloride is described. The overall radio‐chemical yield and specific activity of the former are 53% and 0.53 mCi/mmol and those of the latter are 26% and 0.23 mCi/mmol. The method described is of micromolar scale designed for maintaining cost economy while yielding final products of sufficient radioactivity for in vitro and in vivo metabolism studies.
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## Abstract Two benzodiazepine CCK antagonists __N__‐(2,3‐dihydro‐1‐[^14^C]methyl‐2‐oxo‐5‐phenyl‐1H 1,4‐benzodiazepin‐3‐yl)‐benzamide **2** and __N__‐(2,3‐dihydro‐1‐[^14^C]methyl‐2‐oxo‐5‐phenyl‐1H‐1,4‐benzodiazepin‐3‐yl)‐[^14^C]methyl‐benzamide **3** were synthesized in high yields through the reac