| 摘要 |
The present invention relates to crystalline polymorphs B, C and D of 7-chloro-4-(piperazin-1-yl)quinoline. The polymorph B has an X-ray powder diffraction pattern with the specific peaks at 2-theta=6.95°, 20.40°, 25.80°, 10.30° and 13.70° wherein said values may be ±0.1° 2-theta. The polymorph C has an X-ray powder diffraction pattern with the specific peaks at 2-theta=23.6°, 23.95°, 20.4°, 23.2°, 24.45°, 18.3°, 18.6°, 24.7° and 22.2° wherein said values may be ±0.1° 2-theta. The polymorph D has an X-ray powder diffraction pattern with the specific peaks at 2-theta=18.1°, 19.8°, 16.45°, 17.85°, 23.1°, 24.65°, 20.35° and 27.65° wherein said values may be ±0.1° 2-theta. Said specific peaks have an intensity of at least 30%. The invention further relates to a process for the preparation of the crystalline polymorphs B, C and D of 7-chloro-4-(piperazin-1-yl)quinoline and to the use thereof in the synthesis of piperaquine or one of its pharmaceutically acceptable salts. |
