04-04-2019 дата публикации
Номер: US20190100550A1
The present disclosure provides novel crystalline sofosbuvir form-M3 and a process for the preparation of sofosbuvir form-M3. The crystalline sofosbuvir form-M3 disclosed herein may be useful in the formulation of pharmaceutical dosage forms. 1. Crystalline sofosbuvir form-M3.2. The crystalline sofosbuvir form-M3 of claim 1 , characterized by a PXRD pattern having peaks at 2θ angle positions of 7.61 claim 1 , 16.92 claim 1 , and 20.47±0.2°.3. The crystalline sofosbuvir form-M3 of claim 1 , characterized by a PXRD pattern having peaks at 2θ angle positions of 7.61 claim 1 , 14.19 claim 1 , 16.92 claim 1 , 17.98 claim 1 , 19.58 claim 1 , 20.47 claim 1 , and 23.27±0.2°.4. The crystalline sofosbuvir form-M3 of claim 1 , characterized by a PXRD pattern as shown in .5. A process for the preparation of crystalline sofosbuvir form-M3 claim 1 , comprising the steps of:a. dissolving sofosbuvir in a solvent to form a solution;b. adding an anti-solvent to the solution; andc. isolating crystalline sofosbuvir form-M3.6. The process according to claim 5 , wherein the solvent comprises a water-miscible solvent.7. The process according to claim 6 , wherein the solvent further comprises water.8. The process according to claim 6 , wherein the water-miscible solvent is selected from the group consisting of methanol claim 6 , ethanol claim 6 , isopropanol claim 6 , 1-butanol claim 6 , isobutanol claim 6 , 1-pentanol claim 6 , acetone claim 6 , acetonitrile claim 6 , N claim 6 ,N-dimethylformamide claim 6 , dimethylsulfoxide claim 6 , 1 claim 6 ,2-dimethoxyethane claim 6 , and mixtures thereof.9. The process according to claim 5 , wherein the anti-solvent is water.10. The process according to claim 5 , further comprising the step of stirring after adding anti-solvent and before the isolating step.11. The process according to claim 5 , wherein the solution is seeded with crystalline sofosbuvir form-M3 after adding an anti-solvent and before the isolating step.12. (canceled)13. (canceled) ...
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