1022. Befunolol
Nomenclature
CAS number: 39552-01-7
1-[7-[2-Hydroxy-3-[(1-methylethyl)amino]propoxy]-2-benzofuranyl]ethanone; 7-[2-hydroxy-3-(isopropylamino)propoxy]-2-benzofuranyl methyl
ketone; 2-acetyl-7-(2-hydroxy-3-isopropylaminopropoxy)benzofuran. C16H21NO4; mol wt 291.34.
C 65.96%, H 7.27%, N 4.81%, O 21.97%.
Description and references
β-Adrenergic blocker. Prepn: K. Ito et al., DE 2223184; eidem, US 3853923 (1972, 1974 both to Kakenyaku Kako). Prepn and activity of optical isomers: J. Nakano et al., Chem. Pharm. Bull. 36, 1399 (1988). Determn of befunolol and metabolites in human plasma: K. Kawahara, T. Ofuji, J. Chromatogr. 168, 266 (1979). Absorption, distribution, excretion in rats: H. Kitagawa et al., Oyo Yakuri 17, 383, 393 (1979), C.A. 91, 13374w-5x (1979). General pharmacology: S. Masumoto et al., Iyakuhin Kenkyu 10, 741 (1979), C.A. 92, 88015s (1980). Pharmacodynamics: S. Harada et al., Arch. Int. Pharmacodyn. Ther. 252, 262 (1981).
Properties
Crystals from cyclohexane/acetone, mp 115°. LD50 in mice: 100-105 mg/kg i.v. (Ito).Derivative
Hydrochloride.Nomenclature
CAS number: 39543-79-8
BFE-60; Benfuran (Kaken); Bentos (Kaken); Glauconex (Alcon). C16H21NO4.HCl; mol wt 327.80.
C 58.62%, H 6.76%, N 4.27%, O 19.52%, Cl 10.82%.
Properties
Crystals from ethyl acetate, mp 163°.Derivative
(S)-()-Form hydrochloride.Nomenclature
CAS number: 66717-59-7
Properties
Pale yellow prisms from isopropyl alcohol, mp 151-152°. [α]D 15.5° (c = 1 in methanol).Derivative
(R)-(+)-Form hydrochloride.Nomenclature
CAS number: 66685-79-8
Properties
Pale yellow prisms from isopropyl alcohol, mp 151°. [α]D +15.3° (c = 1 in methanol).Therapeutic Category
Antiglaucoma.
Keywords
β-Adrenergic Blocker; Antiglaucoma