Synthesis of carbon-14 labeled 1, 4-benzodiazepines
✍ Scribed by Richard S. P. Hsi
- Publisher
- John Wiley and Sons
- Year
- 1973
- Tongue
- French
- Weight
- 248 KB
- Volume
- 9
- Category
- Article
- ISSN
- 0022-2135
No coin nor oath required. For personal study only.
✦ Synopsis
Abstract
Reaction of 7‐chloro‐1, 3‐dihydro‐5‐phenyl‐2H‐1, 4‐benzodiazepine ‐2‐thione (Ia) and 7‐chloro‐5‐(2‐chlorophenyl)‐1, 3‐dihydro‐2H, 1, 4‐benzodiazepine‐2‐thione (Ib) with hydrazine produces. respectively, 7‐chloro‐5‐phenyl‐3H‐1, 4‐benzo‐diazepin‐2‐yl hydrazin (IIa) and 7‐chloro‐5(2‐chlorphenyl)‐3H‐1, 4‐benzodiaze‐pin‐d‐ylhydrazine (IIb). Acetylation of IIa and IIb with N‐acetyl ‐ 1^14^C‐imida‐zole affords acetic acid‐1‐^14^C 2‐(7‐chloro‐5‐phenyl‐3H‐1, 4‐benzodiazenpin‐2‐yl) hydrazide (IIIa) and acetic acid‐1‐^14^C 2‐[7‐chloro‐5‐(2‐chlorphenyl) ‐3H‐1, 4‐benzodiazepine‐2‐yl] hydrazide (IIIb). Compounds IIIa and IIIb are thermally cyclised to give 8‐chloro‐1‐methyl‐6‐phenyl‐4H‐s‐triazol [4, 3] [1, 4] benzodiase‐pine‐1‐^14^c (IVa) and 8‐chloro‐6 (2‐chlorophenyl)‐1‐methyl‐4H‐s‐trizolo[4, 3‐a] ‐[1, 4] benzodiazepine ‐1‐^14^C (IVb).
📜 SIMILAR VOLUMES
## Abstract Carbon‐13 and carbon‐14 labeled forms of the title compound have been prepared from the correspondingly labeled forms of 8‐chloro‐1‐methyl‐6‐phenyl‐4H‐__s__‐triazolo[4,3‐a][1,4]benzodiazepine (__3__)Alprazolam is the generic USAN name for this compound. . A modified and more convenient
## Abstract A group of radioactive 1,4‐benzodiazepine derivatives have been synthesized from glycine‐1‐^14^C. The subject compounds are labeled with carbon‐14 in the 2‐position of the 1,4‐benzodiazepine ring system.
## Abstract Two benzodiazepine CCK antagonists __N__‐(2,3‐dihydro‐1‐[^14^C]methyl‐2‐oxo‐5‐phenyl‐1H 1,4‐benzodiazepin‐3‐yl)‐benzamide **2** and __N__‐(2,3‐dihydro‐1‐[^14^C]methyl‐2‐oxo‐5‐phenyl‐1H‐1,4‐benzodiazepin‐3‐yl)‐[^14^C]methyl‐benzamide **3** were synthesized in high yields through the reac
2-14C-oxazepam (z) d 4 C -(+)and -(-1 -7-chloro-l--methyl-5-phenyl-1,3,4,5-tetrahydro-3H-l,4-benzodiazepine-2--one (s and 2) as well as 2-14C-7-chloro-4-carbamoyl-l-methyl--5-phenyl-1,3,4,5-tetrahydro-3H-l,4-benzodiazepine-2-one (9-1 were synthesised from ~arbobenzoxy-glycine-1-~~C. The overall rad