| 摘要 |
1. A process for the synthesis of isoindoline, wherein a solution of phthalonitrile in a solvent selected from tetrahydrofuran, a mixture of tetrahydrofuran/water, or dimethoxyethane, is subjected to a hydrogen pressure of 100 to 180 bars, at a temperature of 30 to 100.degree. C., and in the presence of 5% Pt/C. 2. A process according to claim 1, wherein the solvent is tetrahydrofuran. 3. A process according to claim 1, wherein the solvent is a mixture of tetrahydrofuran/water in which the water content does not exceed 10%. 4. A process according to claim 3, wherein the solvent is a mixture of tetrahydrofuran/water in which the water content does not exceed 5%. 5. A process according to claim 1, wherein the solvent is dimethoxyethane. 6. A process according to claim 1, wherein the hydrogen pressure is from 150 to 180 bars. 7. A process according to claim 1, wherein the temperature is from 50 to 70.degree. C. 8. A process according to claim 1, wherein the amount of Pt/C used is from 10 to 25% of the weight of phthalonitrile employed. 9. A process according to claim 8, wherein the amount of Pt/C used is 20% of the weight of phthalonitrile employed. 10. A process according to claim 1, wherein the amount of 2-methylbenzylamine in the isoindoline obtained does not exceed 1.5%. 11. A process according to claim 10, wherein the amount of 2-methylbenzylamine in the isoindoline obtained does not exceed 0.2%. 12. The use of isoindoline, which is prepared according to any of claims 1-11, in synthesis of 2-(S)-benzyl-4-oxo-4-(cis-perhydroisoindol2-yl)-butyric acid , or pharmaceutically acceptable salts thereof and their hydrates.
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