Title: Bromperidol
CAS Registry Number: 10457-90-6
CAS Name: 4-[4-(4-Bromophenyl)-4-hydroxy-1-piperidinyl]-1-(4-fluorophenyl)-1-butanone
Additional Names: 4-[4-(p-bromophenyl)-4-hydroxypiperidino]-4¢-fluorobutyrophenone
Manufacturers' Codes: R-11333
Trademarks: Azurene (Cilag-Chemie); Impromen (Janssen); Tesoprel (Organon)
Molecular Formula: C21H23BrFNO2
Molecular Weight: 420.32
Percent Composition: C 60.01%, H 5.52%, Br 19.01%, F 4.52%, N 3.33%, O 7.61%
Literature References: Bromine analog of haloperidol, q.v. Prepn (no data): P. A. J. Janssen, GB 895309; idem, US 3438991 (1962, 1969 both to Janssen); C. J. E. Niemegeers, P. A. J. Janssen, Arzneim.-Forsch. 24, 45 (1974). Prepn of 82Br bromperidol and preliminary tissue distribution studies: S. H. Vincent et al., J. Med. Chem. 23, 75 (1980). Pharmacological study: C. J. E. Niemegeers, P. A. J. Janssen, Life Sci. 24, 2201 (1979). Preliminary clinical study: B. Woggon et al., Int. Pharmacopsychiatry 14, 213 (1979). Radioimmunoassay: E. Van Den Eeckhout et al., Eur. J. Drug Metab. Pharmacokinet. 5, 45 (1980).
Properties: Off-white amorphous or microcrystalline powder, mp 155-158°. uv max: 245 nm. pKa 8.6-8.7. Soly in water: 0.09 mg/ml; in 0.1M tartaric, lactic, citric and acetic acids: greater than or equal to 10 mg/ml.
Melting point: mp 155-158°
pKa: pKa 8.6-8.7
Absorption maximum: uv max: 245 nm
Therap-Cat: Antipsychotic.
Keywords: Antipsychotic; Butyrophenones. |