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The synthesis of 7‐chloro‐1‐methyl‐5‐phenyl‐1, 3‐dihydro‐2H‐1,4‐benzodiazepin‐2‐one‐5‐ 14 C and 7‐nitro‐1‐methyl‐5‐(2′‐fluorophenyl)‐1, 3‐dihydro‐2H‐1,4‐benzodiazepin‐2‐one‐5‐ 14 C
Author(s) -
Kaegi H. H.,
Burger W.,
Bader C. J.
Publication year - 1982
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580190215
Subject(s) - chemistry , diazepine , nitro , ring (chemistry) , medicinal chemistry , methyl group , methylation , d 1 , stereochemistry , flunitrazepam , condensation , organic chemistry , benzodiazepine , group (periodic table) , gene , biochemistry , alkyl , receptor , physics , thermodynamics
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 described. This sequence of reactions allows the preparation of the intermediate o ‐methylamino‐benzophenones in good yields.