Osimertinib ketorolac salt crystal form and preparation method thereof

A technology of osimertinib ketorolate and tenidone ketone salt, which is applied in the field of medicine, can solve the problems of high humidity, easy deliquescence, and high hygroscopicity, and achieves simple and easy preparation methods, low hygroscopicity, and high toxicity Effect

Pending Publication Date: 2019-11-22
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Although there are many reports about other salts of osimertinib, the problems of mesylate with high toxicity, high hygroscopicity and high humidity are easy to deliquescence have been improved, but the druggability of these salts needs to be further studied, and there is still a need for further research. Off-the-shelf drugs offer more options

Method used

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  • Osimertinib ketorolac salt crystal form and preparation method thereof
  • Osimertinib ketorolac salt crystal form and preparation method thereof
  • Osimertinib ketorolac salt crystal form and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] N-[2-[[2-(dimethylamino)ethyl](methyl)amino]-4-methoxy-5-[[4-(1-methyl-1H-indole-3- Base) pyrimidin-2-yl] amino] phenyl] prop-2-enamide 5.01g and 5-benzoyl-2,3-dihydro-1H-pyrrolopyrrolidine-1-carboxylic acid 3.58g were added to 30mL In acetone, slowly heat until dissolved, stir for 10 hours, reduce the reaction to 10°C, filter with suction, and dry to obtain a solid with a yield of 94.7% and a purity of 99.9%.

Embodiment 2

[0052] N-[2-[[2-(dimethylamino)ethyl](methyl)amino]-4-methoxy-5-[[4-(1-methyl-1H-indole-3- Base) pyrimidin-2-yl] amino] phenyl] prop-2-enamide 5.01g and 5-benzoyl-2,3-dihydro-1H-pyrrolopyrrolidine-1-carboxylic acid 4.34g were added to 35mL In dichloromethane, heat slowly until dissolved, stir for 9 hours, reduce the reaction to 12°C, filter with suction, and dry to obtain a solid with a yield of 94.1% and a purity of 99.9%.

Embodiment 3

[0054] N-[2-[[2-(dimethylamino)ethyl](methyl)amino]-4-methoxy-5-[[4-(1-methyl-1H-indole-3- Base) pyrimidin-2-yl] amino] phenyl] prop-2-enamide 5.01g and 5-benzoyl-2,3-dihydro-1H-pyrrolopyrrolidine-1-carboxylic acid 5.10g were added to 40mL In methanol, slowly heat until dissolved, stir for 8 hours, reduce the reaction to 15°C, filter with suction, and dry to obtain a solid with a yield of 93.8% and a purity of 99.8%.

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to an osimertinib ketorolac salt crystal form and a preparation method thereof. An X-ray diffraction pattern expressed by 2theta and utilizing Cu-Kalpha radiation, of the crystal form, has characteristic peaks at 4.9+ / -0.2 degrees, 6.4+ / -0.2 degrees, 12.2+ / -0.2 degrees, 21.+ / -0.2 degrees and 22.6+ / -0.2 degrees. Theosimertinib ketorolac crystal form is low in hygroscopicity, simple in preparation process, stable in property and suitable for large-scale production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a crystal form of osimertinib ketorolate and a preparation method thereof. Background technique [0002] If lung cancer patients have EGFR or ALK gene mutations, the use of targeted drugs can obtain better survival benefits. However, the effects of these drugs are generally short-lived, with resistance developing within 9-11 months, which occurs because cancer cells are able to evade treatment with EGFR or ALK inhibitors by mutating and changing the way they grow active. [0003] Osimertinib, developed by AstraZeneca, is a third-generation oral, irreversible, selective EGFR mutation inhibitor that can be used for both activating and resistant mutant EGFR, that is, for patients with advanced non-small cell lung cancer, 50% of acquired resistance to anti-EGFR therapy is caused by the T790M mutation, and osimertinib can render this challenging mutation ineffective. O...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/04C07D487/04A61P35/00A61P29/00A61K31/506A61K31/407
CPCC07D403/04C07D487/04A61P35/00A61P29/00C07B2200/13
Inventor 张贵民翟立海张敏敏路来菊
Owner LUNAN PHARMA GROUP CORPORATION
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