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The preparation of 7-chloro-5-(2-chlorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one-5-14C

✍ Scribed by H. H. Kaegi; W. Burger

Publisher
John Wiley and Sons
Year
1982
Tongue
French
Weight
168 KB
Volume
19
Category
Article
ISSN
0022-2135

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✦ Synopsis

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%.

📜 SIMILAR VOLUMES

The synthesis of 7-chloro-1-methyl-5-phe
The synthesis of 7-chloro-1-methyl-5-phenyl-1, 3-dihydro-2H-1,4-benzodiazepin-2-one-5-14C and 7-nitro-1-methyl-5-(2′-fluorophenyl)-1, 3-dihydro-2H-1,4-benzodiazepin-2-one-5-14C
✍ H. H. Kaegi; W. Burger; C. J. Bader 📂 Article 📅 1982 🏛 John Wiley and Sons 🌐 French ⚖ 393 KB 👁 1 views

## 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

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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

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## 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