The previously reported synthesis of phenobarbital-2-l4C (1) and those of other barbituric acids labeled in the 2-position with carbon-14 (2,3), have employed the base catalysed condensation of the corresponding ester with urea. Although this reaction gives 60-809 yields of various 5,5 dialkyl subst
The synthesis of dimethoxymethyl phenobarbital labeled with 14C
✍ Scribed by Theodore S. T. Wang
- Publisher
- John Wiley and Sons
- Year
- 1977
- Tongue
- French
- Weight
- 190 KB
- Volume
- 13
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
Dimethoxymethyl phenobarbital (DMMP), labeled with ^14^C on the ring and side chains was prepared for drug metabolism studies. The synthesis of DMMP‐ethyl‐1–^14^C (4a) in four steps provided a 43% yield from ethyl‐1–^14^C iodide. The yields of DMMP‐2–^14^C (4b) and DMMP‐dimethylene‐^14^C (4c) were 87.5% and 30% respectively.
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A new procedure has been developed for the synthesis of I4C-labeled glutethimide with an improved yield from K14CN. In this procedure benzyl cyanide prepared from benzyl chloride and K14CN was almost quantitatively monoethylated by an ion-pair extraction method using 50% excess of tetrabutylammonium
Ring-labeled bunolol, df -5 -[3 -(tertbutylamino) -2-hydroxypropoxyJ-3,Cdihydro-l(2ti)-naphthalenone-l-~4C, was synthesized in several steps by initially allowing 3-phenylpropylmag-lJ4C acid was cyclized to a-tetralone-lJ4C. The ring was then oxidized and opened to 4-(2-hydroxyphenyl)butyri~l-~~C ac
## Abstract PHA‐690509, a cyclin‐dependent kinase A inhibitor, has been labelled with carbon‐14. [^14^C]PHA‐690509 was obtained via a three‐step procedure in 10% overall radiochemical yield starting from [^14^C]thiourea **3**. Copyright © 2007 John Wiley & Sons, Ltd.
## Abstract The arylpiperazine PNU‐243922 (**1**) has been labelled with ^14^C. A two‐step sequence starting from the ^14^C labelled alcohol **6a** led to radiochemically pure (>98%) [^14^C]PNU‐243922 with a specific activity of 546 MBq/mmol Copyright © 2002 John Wiley & Sons, Ltd.