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Osimertinib medicinal eutecticum and preparation method thereof

A technology of osimertinib and co-crystal, which is applied in the field of osimertinib co-crystal and its preparation, can solve the problem that the drugability needs to be further studied, and achieves the effects of simple operation, good solubility and low hygroscopicity

Pending Publication Date: 2022-02-22
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Although the existing literature has disclosed many crystal forms of osimertinib, the systematic research on its crystal forms still needs to be perfected, especially the cocrystal of osimertinib
There are many reports about other salts, but their druggability needs to be further studied

Method used

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  • Osimertinib medicinal eutecticum and preparation method thereof
  • Osimertinib medicinal eutecticum and preparation method thereof
  • Osimertinib medicinal eutecticum and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] Add 2.0g osimertinib and 0.65g malic acid into a mixed solvent of 100mL methanol and 8ml purified water, heat to 50°C and stir to dissolve, reflux for 1 hour, slowly cool down to 5°C, then stand for crystallization under temperature control After 60 hours, filter, wash the filter cake with methanol, and dry under vacuum at 50°C for 10 hours to obtain osimertinib-malic acid co-crystal with a yield of 95.33% and a purity of 99.97%.

Embodiment 2

[0079] Add 2.0g osimertinib and 0.80g malic acid into a mixed solvent of 130mL acetone and 10ml purified water, heat to 55°C and stir to dissolve, reflux for 1 hour, slowly cool down to 10°C, then stand for crystallization under temperature control After 65 hours, filter, wash the filter cake with acetone, and vacuum-dry at 60°C for 8 hours to obtain osimertinib-malic acid co-crystal with a yield of 93.67% and a purity of 99.95%.

Embodiment 3

[0081] Add 2.0g osimertinib and 1.07g malic acid into a mixed solvent of 80mL ethanol and 6ml purified water, heat to 60°C and stir to dissolve, reflux for 1 hour, slowly cool down to 15°C, then stand for crystallization under temperature control After 50 hours, filter, wash the filter cake with ethanol, and vacuum-dry at 50°C for 12 hours to obtain osimertinib-malic acid co-crystal with a yield of 91.77% and a purity of 99.92%.

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Abstract

The invention relates to the technical field of crystal form drug molecules and particularly provides an osimertinib eutecticum, a preparation method and application thereof. The medicinal eutecticumum disclosed by the invention is an osimertinib-malic acid eutecticumum, an osimertinib-malonic acid eutecticumum, an osimertinib-vanillic acid eutecticumum or an osimertinib-sorbic acid eutecticumum. According to the invention, the preparation method of the medicinal eutecticum is easy and convenient to operate, the prepared crystal is high in purity, and compared with an existing osimertinib crystal form, the osimertinib crystal form has better solubility and lower hygroscopicity and is more suitable for medicine development.

Description

technical field [0001] The invention relates to the technical field of crystalline drug molecules, in particular to an osimertinib co-crystal and a preparation method and application thereof. Background technique [0002] Osimertinib, chemical name: N-[2-[[2-(dimethylamino)ethyl](methyl)amino]-4-methoxy-5-[[4-(1- Methyl-1H-indol-3-yl)pyrimidin-2-yl]amino]phenyl]prop-2-enamide, English name: N-(2-{[2-(Dimethylamino)ethyl](methyl) amino}-4-methoxy-5-{[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino}phenyl)acrylamide. CAS number: 1421373-65-0, its structural formula is as follows: [0003] [0004] If patients with lung cancer 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, as cancer cells are able to evade the therapeutic activity of EGFR or ALK inhibitors by mutating and changing their growth patterns . [0005] A...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/04C07C59/245C07C55/08C07C51/43A61K31/506A61P35/00
CPCC07D403/04C07C59/245C07C55/08C07C51/43A61P35/00C07B2200/13
Inventor 张贵民翟立海夏祥来郭立红
Owner LUNAN PHARMA GROUP CORPORATION
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