| 摘要 |
<p>A process for preparing alfuzosin or a salt thereof comprising: (a) condensing 4-amino-2- chloro-6,7-dimethoxyquinazoline with 3-methylaminopropionitrile in the presence of a polar aprotic solvent selected from the group consisting of diglyme, dimethyl formamide, t- butanol, hexamethylphosphoramide or mixtures thereof to form N-(4-amino-6,7- dimethoxyquinazol-2-yl)-N-methyl-2-cyanoethylamine (b) hydrogenating the N-(4-amino- 6,7-dimethoxyquinazol-2-yl)-N-methyl-2-cyanoethylamine using a hydrogenating agent under a pressure of less than 10 kg/cm2 to form N-(4-amino-6,7-dimethoxyquinazol-2-yl)- N-methylpropylenediamine and optionally converting the N-(4-amino-6,7- dimethoxyquinazol-2-yl)-N-methylpropylenediamine to an acid addition salt thereof; and (c) converting tetrahydrofuroic acid to an intermediate form and condensing the intermediate form with the N-(4-amino-6,7-dimethoxyquinazol-2-yl)-N-methylpropylenediamine or with the acid addition salt to yield alfuzosin base, and optionally converting alfuzosin base to a salt of alfuzosin.</p> |
