## 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
Synthesis of 1, 3-dihydro-1-methyl-7-nitro-5-phenyl-2H-1, 4-benzodiazepin-2-one-5-14c (nimetazepam-5-14C)
✍ Scribed by A. Yoshitake; Y. Makari; M. Endo
- Publisher
- John Wiley and Sons
- Year
- 1972
- Tongue
- French
- Weight
- 243 KB
- Volume
- 8
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
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 nearly 36%.
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## 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
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
In order to more easily study the absorption, excretion, and distribution patterns of 7-chloro-1 -(cyclopropylmethyl)-5-phenyl-1 H-1,4-benzodiazepin-
## Abstract 7‐Chloro‐5‐(2‐chlorophenyl)‐1,3‐dihydro‐2H‐1,4‐benzodiazepin‐2‐one labeled with carbon‐14 in carbon 5 of the diazepine ring has been synthesized. The compound was prepared in a multistep synthesis from barium carbonate‐^14^C in an overall yield of 23%.