| 摘要 |
1. A process for preparing -{4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl}-2,4-thiazolidinedione thereof or a salt thereof, or a solvate thereof comprising catalytically reducing 5-{4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzylidene}-2,4-thiazolidinedione or a tautomeric form thereof or a salt thereof, or a solvate thereof, wherein the reduction reaction is carried out using a hydrogen pressure above 1.38 bar (20psi), and thereafter if required forming a tautomeric form thereof or a salt thereof, or a solvate thereof. 2. A process according to claim 1, wherein the reaction is carried out using a hydrogen pressure in the range of from 3.45 to 103,5 bar, 4.14 to 103.5 bar, 5.175 to 103.5 bar or 13.8 to 103.5 bar. 3. A process according to claim 1 or claim 2, wherein the reaction hydrogen pressure is in the range of from 4.83 to 69 bar. 4. A process according to any one of claims 1 to 3, wherein the reaction hydrogen pressure is 4.83, 5.175, 34.5 and 69 bar. 5. A process according to any one of claims 1 to 4, wherein the hydrogenation catalyst is a 10% palladium-on-carbon catalyst. 6. A process according to any one of claims 1 to 5, wherein the catalyst loading is 5 to 100%, (%w/w of catalyst to substrate). 7. A process according to any one of claims 1 to 6, wherein the reaction solvent is acetic acid, aqueous acetic acid, an alkanol, an alkanol admixed with an aqueous mineral acid, tetrahydrofuran or tetrahydrofuran admixed with an aqueous mineral. 8. A process according to claim 7, wherein the reaction solvent is acetic acid. 9. A process according to any one of claims 1 to 8, wherein the reaction temperature is in the range of from 80 degree C to 115 degree C. |
