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Synthesis of [3H]tert-butyl 8-chloro-5,6-dihydro-5-methyl-6-oxo-4h-imidazo[1,5-a][1,4]benzodiazepine 3-carboxylate, a selective, high affinity ligand for the diazepam insensitive (DI) subtype of the benzodiazepine receptor

✍ Scribed by Zi-Qiang Gu; Brian R. de Costa; Garry Wong; Kenner C. Rice; Phil Skolnick

Publisher
John Wiley and Sons
Year
1992
Tongue
French
Weight
388 KB
Volume
31
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

The preparation of [^3^H]‐labelled tert‐butyl 8‐chloro‐5,6‐dihydro‐5‐methyl‐6‐oxo‐4H‐imidazo[1,5‐a][1,4]benzodiazepine 3‐carboxylate (TCIB, 6), a high affinity ligands for the diazepam insensitive (DI) subtype of the benzodiazepine receptor (BZR) is described. Synthesis of [^3^H]TCIB was accomplished in 4 steps starting from 5‐chloroisatoic anhydride. Tritium‐label introduction was achieved in the final step by selective catalytic tritiolysis in 62% radiochemical yield with quantitative isotopic incorporation.

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