Phentolamine Mesilate CAS 65-28-1

Phentolamine mesilate (Phentolamine mesylate) is also known as benzamidoline mesylate, Regitine, chemical name: 3-[[(4,5-dihydro-1H-imidazol-2-yl ) methyl] (4-methylphenyl) amino] phenol mesylate, phentolamine mesylate is an α-receptor blocking drug, by blocking α-receptors and indirectly stimulating β-receptors, rapidly Dilate peripheral blood vessels, significantly reduce peripheral vascular resistance, increase peripheral blood volume, and improve microcirculation. Phentolamine mesylate has an excitatory effect on the heart, increasing myocardial contractility, heart rate, and cardiac output. It is mainly used clinically for the treatment of acute heart failure with pulmonary congestion or pulmonary edema, vasospasm disease, cyanosis of the hands and feet, sensuous toxic shock and diagnostic tests for pheochromocytoma, etc. It is also used for premature ventricular beats. Male sexual dysfunction (ED) and female frigidity.

There are multiple synthetic methods of phentolamine mesylate reported in the literature at present, such as condensation of 3-hydroxyl-4-methyldiphenylamine and chloromethylimidazoline hydrochloride in xylene to obtain the crude product of phentolamine hydrochloride , and then use chloroform-ethanol to mix the solvent essence to obtain phentolamine, which becomes mesylate in absolute ethanol, and crystallizes after concentration. However, due to the high toxicity of xylene and high boiling point, and the phentolamine hydrochloride needs to be refined before being used in the next step reaction, the mesylate needs to be concentrated in a solvent for crystallization, the process is complicated, and the yield is low. The method of dissolving phentolamine in water and passing through a silica gel chromatography column, and adjusting the pH value with ammonia water is relatively irritating to the human body, and the industrial production operation is difficult, which is not suitable for large-scale industrial production needs.