## Abstract 2‐Amino‐3,5‐dihydro‐7‐(3‐thienylmethyl)‐[6‐^14^C]‐4H‐pyrrolo [3,2‐d]pyrimidin‐4‐one monohydrochloride ([^14^C]Cl‐1000), a potent purine nucleoside phosphorylase inhibitor, was made in six steps from potassium [^14^C]cyanide. A key step was the reduction of a nitro and a nitrile group wi
Synthesis of 5-ethyl-2-{5-[4-(2-hydroxyethyl)piperazin-1-ylsulfonyl]-2-n-propoxyphenyl}-7-n-propyl-3,5-dihydro-4H-pyrrolo[3,2-d]-[2-14C]pyrimidin-4-one·2 HCl (14C-SK3530·2 HCl)
✍ Scribed by Hyun-Il Shin; Juyoung Lee; Dae-Kee Kim
- Publisher
- John Wiley and Sons
- Year
- 2006
- Tongue
- French
- Weight
- 185 KB
- Volume
- 49
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
HCl) was synthesized through a straightforward six-step sequence from the readily available [ 14 C-carbonyl]methyl salicylate (2). The overall radiochemical yield of the 1 . 2 HCl from 2 was 10.5%, and its radiochemical purity was 98.8%.
📜 SIMILAR VOLUMES
## Abstract Two benzodiazepines, Diazepam and Flunitrazepam, labeled with carbon‐14 in position 5 of the diazepine ring have been synthesized. Use of a condensation between iminochlorides and ^14^C‐benzonitriles, followed by exhaustive methylation of the resulting quinazolines and hydrolyses is des
## Abstract 7‐Chloro‐1,3‐dihydro‐5‐(2‐fluorophenyl)‐1‐methyl‐2H‐1,4‐benzodiazepin‐2‐one (Fludiazepam) (I), an anti‐anxiety agent, was labelled with carbon‐14 at C‐5 position for metabolic studies. The reaction sequence for the synthesis is shown in Fig. 2. o‐Fluorobenzoic‐^14^C acid (IV) was prepar
The carbon-I4 labelled compound ( 5 ) of 2-[4-(diphenylmethy1)-l -piperazinyl]ethyl methyl (?)-I ,$-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate dihydrochloride (CV-4093 (2HCI)) was synthesized for the study of its metabolism and distribution in test animals. Starting from the co
Tema~epam-2-'~C, 7-Chloro-1,3-ihydro-3-hydroxy-1 -methyl-5-phenyl-2H-1,4-benzodiazepin-2-one--"C, was prepared in a f ive-step synthesis. Chl~roacetic-l-~~C acid was converted to the acid chloride with thionyl chloride. The acid chloride was allowed to react with 2-methylamino-5-chloro-benzophenone
## Abstract The synthesis from carbon‐^14^C dioxide of 1, 3‐dihydro‐1‐methyl‐7‐nitro‐5‐phenyl‐2H‐1, 4‐benzodiazepin‐2‐one‐5‐^14^C (I) for use in metabolic studies has been described. The synthesis was achieved by the sequence shown in figure 1. The overall yield of labelled nimetazepam (I) was near