| 摘要 |
<p>Disclosed is 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-2cyanoethylamine (b) hydrogenating the N-(4-amino-6,7-dimethoxyquinazol-2-yl)-N-methyl-2cyanoethylamine using a hydrogenating agent under a pressure of less than 10 kilograms per centimetre squared to form N-(4-amino-6,7-dimethoxyquinazol-2-yl)-N-methylpropylenediamine and (c) converting tetrahydrofuroic acid (VI) to an intermediate form (VII) and condensing the intermediate form (VII) with the N-(4-amino-6,7-dimethoxyquinazol-yl)- N-methylpropylenediamine or with the acid addition salt thereof to yield alfuzosin base wherein R is defined in the specification.</p> |
