4589. Halazepam

Nomenclature

CAS number: 23092-17-3
7-Chloro-1,3-dihydro-5-phenyl-1-(2,2,2-trifluoroethyl)-2H-1,4-benzodiazepin-2-one; Sch-12041; Paxipam (Schering).
C17H12ClF3N2O; mol wt 352.74.
C 57.88%, H 3.43%, Cl 10.05%, F 16.16%, N 7.94%, O 4.54%.

Description and references

Polyfluoroalkyl analog of diazepam, q.v. Prepn: J. G. Topliss, US 3429874 (1969 to Schering); M. Steinman et al., J. Med. Chem. 16, 1354 (1973). Pharmacology: J. B. Petel et al., Psychopharmacology 61, 25 (1979). Use in schizophrenia: K. Y. Ota et al., Curr. Ther. Res. 15, 327 (1973); in anxiety: K. Rickels et al., Int. Pharmacopsychiatry 13, 118 (1978).

Chemical structure

Properties

Crystals from acetone-hexane, mp 164-166°. LD50 in mice: >4000 mg/kg orally (Steinman).

Note

This is a controlled substance (depressant): 21 CFR, 1308.14.

Therapeutic Category

Anxiolytic.

Keywords

Anxiolytic; Benzodiazepine Derivatives