4213. Flutoprazepam

Nomenclature

CAS number: 25967-29-7
7-Chloro-1-(cyclopropylmethyl)-5-(2-fluorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one; KB-509; ID-1937; Restar (Sumitomo); Restas (Kanebo).
C19H16ClFN2O; mol wt 342.79.
C 66.57%, H 4.70%, Cl 10.34%, F 5.54%, N 8.17%, O 4.67%.

Description and references

Benzodiazepine derivative. Prepn: H. Yamamoto et al., GB 1253368; eidem, US 3925364 (1971, 1975 both to Sumitomo). New process: T. Okamoto et al., DE 2151540; eidem, US 3832344 (1972, 1974 both to Sumitomo). Stability and degradation mechanism in aqueous solns: K. Akimoto et al., Int. J. Pharm. 3, 109 (1979). Pharmacokinetics and metabolism: A. Kozaki et al., Yakugaku Zasshi 102, 1177 (1982), C.A. 98, 119080q (1983). Pharmacology of flutoprazepam and metabolites: K. Oki et al., Arch. Int. Pharmacodyn. Ther. 269, 180 (1984). Acute toxicity study: H. Takebe et al., Oyo Yakuri 20, 1055 (1980), C.A. 95, 73630b (1981).

Chemical structure

Properties

Crystals, mp 118-122°. LD50 in male, female mice, rats (mg/kg): 2640, 2430, 13760, 10060 orally; 2400, 2110, 2460, 2230 i.p.; >5000 s.c. all species (Takebe).

Therapeutic Category

Anxiolytic.

Keywords

Anxiolytic; Benzodiazepine Derivatives