Hubbry Logo
search
logo
1434652

Befunolol

logo
Community Hub0 Subscribers
Write something...
Be the first to start a discussion here.
Be the first to start a discussion here.
See all
Befunolol

Befunolol (INN) is a beta blocker with intrinsic sympathomimetic activity used in the management of open-angle glaucoma. It also acts as a β adrenoreceptor partial agonist. Befunolol was introduced in Japan in 1983 by Kakenyaku Kako Co. under the trade name Bentos.

The first reported synthesis of befunolol in 1974 used a benzofuran derivative (4) with epichlorohydrin and then isopropylamine to add the sidechain which was known to produce beta blockers, by analogy with drugs discovered by Imperial Chemical Industries, such as propanolol. The requisite intermediate was synthesized from ortho-vanillin (1) by a condensation reaction with chloroacetone (2) in the presence of potassium hydroxide, giving 2-acetyl-7-methoxybenzofuran (3), which was demethylated using hydrobromic acid.

See all
User Avatar
No comments yet.