Befunolol Property

Melting point:

115°

Boiling point:

433.35°C (rough estimate)

Density 

1.1049 (rough estimate)

refractive index 

1.5500 (estimate)

storage temp. 

Hygroscopic, -20°C Freezer, Under inert atmosphere

solubility 

Chloroform (Slightly), DMSO (Slightly, Heated)

form 

Solid

color 

White to Off-White

CAS DataBase Reference

39552-01-7

Safety

Toxicity

LD50 in mice: 100-105 mg/kg i.v. (Ito)

Hazard and Precautionary Statements (GHS)

Befunolol Chemical Properties,Usage,Production

Originator

Bentos,Kakenyaku Kako,Japan,1983

Uses

Befunolol is a β-adrenergic blocker with an intrinsic sympathomimetic action. But it can work as a β-adrenergic partial agonist in isolated organs.

Uses

β-Adrenergic blocker used as antiglaucoma agent in ophthalmie solutions

Definition

ChEBI: Befunolol is a member of benzofurans.

Manufacturing Process

To 8.8 g of 2-acetyl-7-hydroxybenzofuran were added 80 ml of epichlorohydrin and 0.2 g of piperidine hydrochloride and the mixture was heated at 105°C for 3 hours. After the reaction, the excess of epichlorohydrin was evaporated and the resultant was distilled under reduced pressure to give 9.3 g of 2-acetyl-7-(2,3-epoxypropoxy)benzofuranhaving a boiling point of 175° to 176°C/0.7 mm Hg. 6 g of the product was dissolved in 30 ml of ethanol and to the solution was added 10 ml of isopropylamine. After refluxing the mixture for 40 minutes, the solvent was evaporated from the reaction mixture. The resulting residue was recrystallized from cyclohexane-acetone to give 6 g of 2-acetyl-7-(2-hydroxy-3-isopropylaminopropoxy)benzofuran having a melting point of 115°C.

Therapeutic Function

Beta-adrenergic blocker

Contact allergens

Befunolol was implicated in allergic contact dermatitis due to beta-blocker agents in eye-drops. Crosssensitivity has been described with levobunolol.