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【结 构 式】 
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【药物名称】Phentolamine mesilate, Z-Max, Vasofem, Vasomax, Regitin 【化学名称】3-[N-(2-Imidazolin-2-ylmethyl)-N-(4-methylphenyl)amino]phenol methanesulfonate 【CA登记号】65-28-1, 50-60-2 (free base) 【 分 子 式 】C18H23N3O4S 【 分 子 量 】377.46571 |
【开发单位】Novartis (Originator), Zonagen (Licensee) 【药理作用】Disorders of Sexual Function and Reproduction, Treatment of, ENDOCRINE DRUGS, RENAL-UROLOGIC DRUGS, Treatment of Erectile Dysfunction, Treatment of Female Sexual Dysfunction, Treatment of Male Sexual Dysfunction, alpha-Adrenoceptor Antagonists |
合成路线1
The condensation of N-(3-hydroxyphenyl)-N-(4-methylphenyl)amine (I) with 2-(chloromethyl)-4,5-dihydro-1H-imidazole (II) by heating at 150-60 C without solvent or in o-dichlorobenzene gives phentolamine as hydrochloride salt (III), which is treated with ammonia to obtain the free base, and finally salified with methanesulfonic acid in ethanol.
| 【1】 Miescher, K.; Marxer, A.; Urech, E.; 2-Aminoalkyl-imidazoline. Helv Chim Acta 1950, 33, 5, 1386-407. |
| 【2】 Miescher, K.; Marxer, A.; Urech, E. (Novartis Corp.); 2-(N,N-Diphenyl-aminomethyl)imidazoles. US 2503059 . |