Phentolamine hydrochloride is Tan Solid
anesthetic (local); inhibitor of DRG IA/Kv4.2 current
Phentolamine Hydrochloride ia an adrenergic blocking agent. An antihypertensive. Used for the treatment of pheochromocytoma.
Phentolamine hydrochloride is an adrenergic blocking agent. An antihypertensive. Used for the treatment of pheochromocytoma.
199.24 parts of N-(p-methylphenyl)-m'-hydroxyphenylamine and 77.52 parts of 2-chloromethylimidazoline hydrochloride are heated for sixteen hours in an oil bath having a temperature of 150°C, while stirring and introducing a current of nitrogen. The viscous contents of the flask are then cooled to about 100°C, mixed with 400 parts by volume of hot water, and stirred for a short time.
After further cooling to about 60°C, 200 parts by volume of water and 500 parts by volume of ethyl acetate at 60°C are added, and the aqueous layer is separated. The excess of starting material may be recovered from the ethyl acetate.
The aqueous portion is chilled in a cooling chamber at -10°C, whereupon the hydrochloride of 2-[N-(p-methylphenyl)-N-(m'-hydroxyphenyl)-aminomethyl]imidazoline crystallizes. Upon being concentrated and cooled the mother liquor yields a further quantity of the hydrochloride. The combined quantities of hydrochloride are treated with a small quantity of cold water, dried with care, and washed with ethyl acetate. The product is then crystallized from a mixture of alcohol and ethyl acetate, and there is obtained a hydrochloride melting at 239°-240°C.
Regitine Hydrochloride (Ciba-Geigy).
α-adrenoceptor antagonist; peripheral vasodilator.
