Polymorphic forms of dasatinib
A dasatinib form technology, applied in the field of co-crystal and solvate of dasatinib and its preparation, can solve uneconomical problems
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Embodiment 1a
[0910] Example 1a: (using DMAc and methanol as solvent) Preparation of Dasatinib-thymine co-crystal of formula Ia from II-one-pot synthesis method
[0911]
Embodiment -1b
[0912] Add Formula II (2.00g, 0.0051mol, 1.00 equivalent), Formula III (6.00mL, 3.00vol) and N, N-dimethylacetamide ( 2.00mL, 1.00vol) and heat the material to 75±2°C. Maintain the reaction mass at 75±2°C under stirring. The resulting reaction mass (containing formula I) was cooled to 25±5°C, and thymine (0.96g, 0.007mol, 1.50 equivalent) was added to the reaction mass at 25±5°C under stirring. Under stirring, methanol (60.0 mL, 30.0 vol) was added to the reaction mass at a constant rate at 25±5°C. The material is heated to 60±2°C, and the resulting suspension is maintained at the same temperature under stirring. Cool the material to 25±5°C and maintain the same temperature. Water (15 mL, 7.50 vol) was added to the reaction mass at a constant rate with stirring. Maintain the reaction mass at 25±5°C. The material was filtered, and the solid was washed with methanol (10.0 mL, 5.00 vol), sucked dry and dried under vacuum at 50±5°C to obtain the dasatinib-thymine co-crystal of...
Embodiment -1c
[0916] Add formula II (50.00g, 0.127mol, 1.00 equivalent), formula III (150mL, 3.00vol) and N, N-dimethylacetamide (50.0 vol) to a 3L glass container equipped with a stirrer, condenser and thermometer probe. mL, 1.00vol) and heat the material to 75±5°C. Maintain the reaction mass at 75±5°C under stirring. The resulting reaction mass was cooled to 25±5°C, and adenine (25.7g, 0.190mol, 1.50 equivalent) was added to the reaction mass at 25±5°C under stirring. Under stirring, methanol (1500 mL, 30.0 vol) was added to the reaction mass at a constant rate at 25±5°C. The material is heated to 60±2°C, and the resulting suspension is maintained at the same temperature under stirring. Cool the material to 25±5°C and maintain the same temperature. Water (650 mL, 13.0 vol) was added to the reaction mass at a constant rate with stirring. Maintain the reaction mass at 25±5°C. The material was filtered, and the solid was washed with methanol (350 mL, 7.00 vol), sucked dry, and dried unde...
PUM
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