Novel alprenolol derivative

Abstract

Abstract NEW MATERIAL:The compound of formula I (R is group of formula II, formula III, etc.) and its hydrochloride. EXAMPLE:Butanedioic acid mono[1-{(2-allylphenoxy)methyl}-{2-(1-methylethyl) amino}ethyl] ester hydrochloride. USE:A compound effective in improving the bioavailability of alprenolol useful as a beta-blocker. It is absorbed through digestive tracts by oral administration, transferred to blood without being affected by 1st passage through the liver and converted into alprenolol. PREPARATION:The compound of formula I can be produced either by bonding alprenolol with succinic anhydride, glutaric anhydride or maleic anhydride through ester bond or by bonding alprenolol with glutaric anhydride through ester bond and reacting the product with an ethyl halide.

Inventors

• 👤 Shinichi Shimada
• 👤 Noboru Kawaguchi
• 👤 Tadayoshi Koyama
• 👤 Akinori Wakao
• 👤 Keiji Hayashi
• 👤 Yasuyoshi Takeshita
• 👤 Masamichi Nakakoshi
• 👤 Norio Kawanishi

Bibliographic Details