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1. WO2011050826 - PROCÉDÉ DE FABRICATION D'UNE FORME CRISTALLINE DE LINÉZOLIDE

Note: Texte fondé sur des processus automatiques de reconnaissance optique de caractères. Seule la version PDF a une valeur juridique

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Claims

1. A process for making a crystalline linezolid, comprising a step of dissolving linezolid in an organic solvent to obtain a solution followed by a step of adding the obtained solution into an antisolvent kept at a pre-selected temperature and seeded with crystals of the desired crystalline form of linezolid.

2. The process according to claim 1 , wherein the crystalline linezolid is the Form A of linezolid characterised by a XRPD powder diffraction pattern comprising the peaks at about 7.6,

9.6, 13.6, 14.9, 18.2, 18.9, 21.2, 22.3, 25.6, 26.9, 27.9 and 29.9 degrees 2 theta, when measured with CuKal radiation (λ = 1.54060 A).

3. The process according to claim 1-2, wherein the organic solvent is selected from an aliphatic alcohol, such as methanol, ethanol and isopropanol, a cyclic ether, such as 1 ,4-dioxane, and an aliphatic ester, such as ethyl acetate, and mixtures thereof.

4. The process according to claims 1-3, wherein the temperature of the solution is within the range from 50 °C up to the reflux temperature.

5. The process according to claims 1-4, wherein the concentration of the linezolid in the solution is within a range of between 10-100 ml of the solvent per 1 gram of linezolid.

6. The process according to claims 1-5 wherein the antisolvent is an aliphatic

hydrocarbon, preferably with 5 to 10 carbon atoms, and/or an aliphatic ether, preferably that of 4 to 10 carbon atoms.

7. The process according to claim 6, wherein the hydrocarbon is a hexane such as n-hexane, a heptane such as n-heptane, cyclohexane and/or petroleum ether, the aliphatic ether is methyl-/ert. -butyl ether; and mixtures thereof.

8. The process according to claims 1-7, wherein the pre-selected temperature of the antisolvent is within the range from -20°C to +25°C, preferably at a temperature lower than 0°C.

9. The process according to claims 1-8, wherein the mutual ratio between the antisolvent and the solvent is from 1 : 1 to 10 : 1 (v/v), advantageously from 2 : 1 to 7 : 1 (v/v) .

10. The process according to claims 1-9, wherein the antisolvent is seeded with crystals of the crystalline Form A of linezolid.

1 1. The process according to claims 1-10, wherein the relative amount of the seeds in respect to the weight of the linezolid in the solution is 1- 25 %.

12. The process according to claims 1-1 1 , wherein the crystallization provides a precipitate of the crystalline Form A of linezolid, which is essentially free from any other crystalline form of linezolid.