4604. Haloxazolam

Nomenclature

CAS number: 59128-97-1
10-Bromo-11b-(2-fluorophenyl)-2,3,7,11b-tetrahydrooxazolo[3,2-d][1,4]benzodiazepin-6(5H)-one; CS-430; Somelin (Sankyo).
C17H14BrFN2O2; mol wt 377.21.
C 54.13%, H 3.74%, Br 21.18%, F 5.04%, N 7.43%, O 8.48%.

Description and references

Sleep-inducing agent, related structurally to oxazolam and cloxazolam, q.q.v. Prepn of analogous compounds: T. Miyadera et al., J. Med. Chem. 14, 520 (1971). Structure-activity study: M. Yoshimoto et al., Chem. Pharm. Bull. 25, 1378 (1977). Pharmacological studies: T. Kamioka et al., Arzneim.-Forsch. 28, 838 (1978). Metabolism in animals: R. Hayashi et al., Oyo Yakuri 17, 617 (1979), C.A. 91, 204161s (1979).

Chemical structure

Properties

Colorless cryst, mp 185°. Sparingly sol in water. LD50 in mice: 1850 mg/kg orally (Kamioka).

Note

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

Therapeutic Category

Sedative, hypnotic.

Keywords

Sedative/Hypnotic; Benzodiazepine Derivatives