Bevantolol hydrochloride

Bevantolol hydrochloride is a moderately lipophilic, long-acting, cardioselective -adrenoceptor blocker. It has no ISA but has membrane-stabilizing activity. The dmg is in use in Europe for the treatment of hypertension and angina. It is rapidly absorbed from the GI tract. Peak plasma levels occur in 1—2 h. It is metabolized extensively in the Hver to a metaboHte that has some ISA. It is excreted by the Hver and the kidneys and excretion is delayed in patients having kidney failure. 

The reactor and filter are rinsed with 186 L of isopropyl alcohol and 2.7 kg of anhydrous hydrogen chloride is added to the combined filtrate. The batch is heated to reflux for 2 hours. The temperature is adjusted to 65°C and the solution is seeded with bevantolol hydrochloride crystals. The mixture is held at this temperature with stirring until a heavy sand-like slurry is present. The mixture is allowed to cool to ambient temperature without stirring or artificial cooling. It is then cooled to 20°C. The slurry is centrifuged and the product rinsed with isopropyl alcohol until the filtrate is colorless. After being vacuum dried at 50-55°C the product is milled if necessary yield of bevantolol hydrochloride 22.7 kg (78.6%) melting point 137-138°C. 

Neah, S.H. Shinwari, M.K. Hellmuth, E.W. Melting point phase diagrams of free base and hydrochloride salts of bevantolol, pindolol and propanolol. Int. J. Pharm. 1993, 99, 303-310. 

---