SUSTAINABLE CRYSTALLINE MODIFICATIONS OF CHLORIDE DOTAP Russian patent published in 2017 - IPC C07C219/08 A61K47/18 A61K9/127 

FIELD: chemistry.

SUBSTANCE: invention relates to a method of manufacturing crystalline form of chloride (2R, S)-, (2S)- or (2R)-DOTAP (N, N, N-trimethyl-2,3-bis [[(9Z) -1-oxo -9-octadecenyl] oxy]-1-propanamide chloride). The process comprises crystallization chloride (2R, S)-, (2S)- or (2R)-DOTAP of one or more aprotic solvents, wherein the crystallisation takes place by cooling slowly from 35°C to -12°C for constituting 12 hours, or by slowly cooling from a temperature lower than the time period 35°. C over a period of time ranging from 10 to 50 parts crystalline chloride (2R, S)-DOTAP has one of the following characteristics: the values 2 theta, including at least the values constituting 12.6, 19.5, 20.2, 21.5 and 25.2; or 2 theta values, comprising at least the values of 6.5, 12.6, 13.4, 19.5, 20.2, 21.5, 25.2 and 29.8; or an X-ray powder diffraction, the diffraction pattern corresponding to FIG. 1. Crystalline chloride (2S)-DOTAP has one of the following characteristics: the values 2 theta, including at least the values constituting 12.8, 19.5, 19.8, 20.2 and 21.6; 2 theta values, comprising at least the values of 6.5, 12.8, 19.5, 19.8, 20.2, 20.7, 21.6 and 25.3; or an X-ray powder diffraction, the diffraction pattern corresponding to FIG. 2. Crystalline chloride (2S)-DOTAP has one of the following characteristics: the values 2 theta, including at least the values constituting 12.8, 19.5, 19.8, 20.2 and 21.6; 2 theta values, comprising at least the values of 6.5, 12.8, 19.5, 19.8, 20.2, 20.7, 21.6 and 25.3; or an X-ray powder diffraction, the diffraction pattern corresponding to FIG. 3. X-ray powder diffractometry was carried out using Cu as a radiation source.

EFFECT: proposed method allows to obtain crystalline forms of chloride with improved stability and purity.

8 cl, 12 dwg, 5 tbl, 5 ex