CRYSTAL OF 3,5-DISUBSTITUTED BENZENE ALKYNYL COMPOUND

• Main Author: EGAMI, Kosuke
• Format: Patent
• Language: English; French; German
• Published: 24.06.2020
• Subjects: AFTER-TREATMENT OF SINGLE CRYSTALS OR A HOMOGENEOUSPOLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; APPARATUS THEREFOR; CHEMISTRY; CRYSTAL GROWTH; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; PRODUCTION OF A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITHDEFINED STRUCTURE; REFINING BY ZONE-MELTING OF MATERIAL; SINGLE CRYSTALS OR HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITHDEFINED STRUCTURE; SINGLE-CRYSTAL-GROWTH; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; UNIDIRECTIONAL SOLIDIFICATION OF EUTECTIC MATERIAL ORUNIDIRECTIONAL DEMIXING OF EUTECTOID MATERIAL

An object of the present invention is to provide a crystal of (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)-1-pyrrolidinyl)-2-propen-1-one, which is useful as an antitumor agent, the crystal being stable, excellent in oral absorbability, highly chemically pure, and suitable for mass production. The present invention provides a crystal of (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)-1-pyrrolidinyl)-2-propen-1-one that exhibits an X-ray powder diffraction spectrum containing at least three characteristic peaks at diffraction angles (2¸±0.2°) selected from 9.5°, 14.3°, 16.7°, 19.1°, 20.8°, 21.9°, and 25.2°. The present invention also provides a crystal of (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)-1-pyrrolidinyl)-2-propen-1-one that exhibits an X-ray powder diffraction spectrum containing at least seven characteristic peaks at diffraction angles (2 ¸ ±0.2°) selected from 13.5°, 17.9°, 19.5°, 20.6°, 22.0°, 22.6°, 23.3°, 23.7°, and 24.2°.