SYNTHESIS OF [H-3] 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

被引：7

作者：

GU, ZQ ^{[1
]}

DECOSTA, BR ^{[1
]}

WONG, G ^{[1
]}

RICE, KC ^{[1
]}

SKOLNICK, P ^{[1
]}

机构：

[1] NIDDKD, NEUROSCI LAB, BETHESDA, MD 20892 USA

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 1992年 / 31卷 / 12期

关键词：

IMIDAZOBENZODIAZEPINE; DIAZEPAM INSENSITIVE; BENZODIAZEPINE RECEPTOR; RO-15-4513; TRITIUM LABELING; GABA(A)-RECEPTOR;

D O I：

10.1002/jlcr.2580311213

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

The preparation of [H-3]-labelled tert-butyl 8-chloro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine 3-carboxylate (TClB, 6), a high affinity ligand for the diazepam insensitive (DI) subtype of the benzodiazepine receptor (BZR) is described. Synthesis of [H-3]TClB 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.

引用

页码：1049 / 1055

页数：7

共 25 条

[1] SYNTHESIS OF [H-3]-1-[1-(3-ISOTHIOCYANATOPHENYL)CYCLOHEXYL]PIPERIDINE (METAPHIT), AN ACYLATING AGENT FOR PHENCYCLIDINE RECEPTORS [J].