| 摘要 |
1. Process for the preparation of amlodipine benzenesulphonate of formula (I) characterised by reacting benzenesulphonic acid with phthalamidic acid derivatives of general formula (II): wherein X represents hydrogen or alkali metal or alkali earth metal or quaternary ammonium. 2. A process according to claim 1, characterised in that the phthalamidic acid derivative of general formula (II), wherein X is as defined in claim 1-is reacted with at least a stoichiometric amount or with a small excess of benzenesulphonic acid. 3. A process according to claims 1 or 2, characterised in that the reaction was carried out in an inert solvent at an elevated temperature. 4. Phthalamidic acid derivative of general formula (II): wherein X represents hydrogen or alkali metal or alkali earth metal or quaternary ammonium. 5. 2-[/2-N-(2-carboxy-benzoyl)-aminoethoxy/methyl]-4-(2-chlorophenyl)-3-ethoxy-carbonyl-5-methoxycarbonyl-6-methyl-1,4-dihydropyridine. 6. Process for the preparation of phthalamidic acid derivatives of general formula (II), wherein X represents hydrogen or alkali metal or alkali earth metal or quaternary ammonium, characterized by reacting 4-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-2-(2-phthalimidoethoxy) methyl-1,4-dihydropyridine with a strong base, if desired, reacting the obtained compound of general formula (II), wherein X represents alkali metal or alkali earth metal or quaternary ammonium-with or without isolation with an acid. 7. Process according to claim 6, characterised in that the strong base is alkali metal hydroxide, alkali earth metal oxide or hydroxide, or quaternary ammonium base. 8. Process according to claims 6 or 7, characterised in that the strong base is used in an amount of at least a stoichiometric or a slight excess, and, if desired, neutralized with a stoichiometric amount of acid. 9. Process according to any of claims 6 to 8, characterised in that the reaction with the strong base is carried out at room temperature and the reaction with the acid is carried out during ice-cooling. 10. Process according to claim 1, characterised in that the phthalamidic acid derivative is prepared according to any one of claims 6 to 9.
|
