The preparation of [3H]-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 [3H]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.

[3H]TCIB is a selective, high affinity ligand for the diazepam insensitive subtype of the benzodiazepine receptor, with a radiochemical yield of 62%.

Journal of Labelled Compounds and Radiopharmaceuticals

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

Paper

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

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