A Review of the Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model

<div>Synthesis of 8-substituted imidazobenzodiazepine bivalent ligands.<i> Reagents and Conditions</i>. (a) DMSO, 180°C, 90%; (b) bromine, sodium acetate, and acetic acid, r.t., 80%; (c) LDA, THF, and diethyl chlorophosphate, 0°C; (d) LDA, THF, and ethyl isocyanoacetate; (e) trimethylsilyl acetylene, Pd(OAc)<sub>2</sub>(PPh<sub>3</sub>)<sub>2</sub>, triethylamine, acetonitrile, and reflux, 80%; (f) tetrabutylammonium fluoride, THF, and H<sub>2</sub>O, r.t., 88%; (g) 2N NaOH and ethanol, 70°C, 90%; (h) CDI, DMF, HO(CH<sub>2</sub>)<sub>3</sub>OH, and DBU, 60%; (i) Pd/C, H<sub>2</sub>, ethanol, and DCM, 90%.</div>

International Journal of Medicinal Chemistry

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Scheme 2

Scheme 2: A Review of the Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model 