Afurolol

Originator

Afurolol ,ZYF Pharm Chemical

Manufacturing Process

A mixture of 18.0 g (0.12 mole) 7-hydroxyphthalide, 180.0 g of 1-chloro-2,3- epoxypropane (2 moles) and 0.5 ml of piperidine is heated at 100°C for about 5 h and then the unreacted 1-chloro-2,3-epoxypropane is distilled off in vacuum to yield 12.0 g (48%) of 7-(2,3-epoxypropoxy)phthalide, melting point 88°-90°C, (crystallized successively from methanol and ethyl acetate).
The 7-(2,3-epoxypropoxy)phthalide is dissolved in methanol and t-butylamine are added to the solution at about 20°C. The solution is allowed to stand overnight and, the mixture is evaporated in vacuum and the residue is dried to give 7-(2-hydroxy-3-t-butylamino-propoxy)phthalide.

Therapeutic Function

Beta-adrenergic blocker