2S,3R)-2-[3-(4-Fluorophenyl)]propylamino-3-(3,4-di hydroxyphenyl)-3-hydroxypropionic acid pyrrolidine amide hydrobromide (SM-11044) was labeled with carbon-14 for use in mammalian metabolic studies. The synthesis was achieved according to the scheme shown in Fig. 5. Grignard reaction of 3,4-methylen
The synthesis of [14C]BRL 26830a, a novel β-adrenoceptor agonist
✍ Scribed by R. Freer; D. J. Morecombe
- Publisher
- John Wiley and Sons
- Year
- 1992
- Tongue
- French
- Weight
- 480 KB
- Volume
- 31
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
BRL 26850A has been extensively reported ^1^ as a novel β‐adrenoceptor agonist. In order to perform metabolism studies, carbon‐14 radiolabelled BRL 26830A was synthesised from potassium [^14^C]cyanide. As BRL 26830A contains two asymmetric centres, the initial product required resolution of the two enantiomeric pairs. This was achieved by sequential fractional crystallisation of the free base and then the hydrobromide salt to obtain the required (R^*^, R^*^)‐(+) enantiomeric pair before final conversion to the hemifumarate salt ([^14^C]BRL 26830A).
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## SUM MARY A ''C-labelled form of 2-chloro-K[(R)-(2-benzoxazolyl)thio-2-propyl]adenosine a, a novel antiischaemic adenosine A, agonist, has been prepared in three steps from [8- '4C]-9-(2,3,5-tri-0-benzoyl-~-D-ribofuranosyl)-2,6-dichloropurine a. The overall radiochemical yield was 56%. The radio