Bentos,Kakenyaku Kako,Japan,1983
β-Adrenergic blocker used as antiglaucoma agent in ophthalmie solutions
Befunolol is a β-adrenergic blocker with an intrinsic sympathomimetic action. But it can work as a β-adrenergic partial agonist in isolated organs.
ChEBI: Befunolol is a member of benzofurans.
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.
Befunolol was implicated in allergic contact dermatitis
due to beta-blocker agents in eye-drops. Crosssensitivity
has been described with levobunolol.
