Title: Doxefazepam
CAS Registry Number: 40762-15-0
CAS Name: 7-Chloro-5-(2-fluorophenyl)-1,3-dihydro-3-hydroxy-1-(2-hydroxyethyl)-2H-1,4-benzodiazepin-2-one
Additional Names: N-1-hydroxyethyl-3-hydroxyflurazepam
Manufacturers' Codes: SAS-643
Trademarks: Doxans (Schiapparelli)
Molecular Formula: C17H14ClFN2O3
Molecular Weight: 348.76
Percent Composition: C 58.55%, H 4.05%, Cl 10.17%, F 5.45%, N 8.03%, O 13.76%
Literature References: Prepn: G. F. Tamagnone et al., Arzneim.-Forsch. 25, 720 (1975); eidem, J. Pharm. Pharmacol. 26, 566 (1974); F. De Marchi, G. F. Tamagnone, DE 2338058 (1974 to Schiapparelli), C.A. 80, 121016v (1974). Comparison with flurazepam, q.v., and pharmacology, toxicity studies: M. Babbini et al., Arzneim.-Forsch. 25, 1294 (1975). Structure-activity studies: eidem, Pharmacol. Res. Commun. 7, 337 (1975). GC determn in blood and tissue: F. Marcucci et al., J. Chromatogr. 198, 180 (1980); in plasma, urine: S. Mardente et al., Ther. Drug Monit. 3, 351 (1981). Quantitative EEG, behavioral effects: W. G. Sanita et al., ibid. 341. Effect on sleep: G. Rodriguez et al., Neuropsychobiology 11, 133 (1984).
Properties: Crystals from methylene chloride/petr ether, mp 138-140°. LD50 in rats, mice (mg/kg): 2550, >1500 orally; 586, 774 i.p. (Babbini).
Melting point: mp 138-140°
Toxicity data: LD50 in rats, mice (mg/kg): 2550, >1500 orally; 586, 774 i.p. (Babbini)
Therap-Cat: Sedative, hypnotic.
Keywords: Sedative/Hypnotic; Benzodiazepine Derivatives. |