Novel crystal form of EGFR inhibitor, and preparation method thereof

A crystal form, 90%RH-95%RH technology, applied in the field of medicinal chemistry, can solve problems that have not yet been discovered, and achieve the effects of low toxicity, good repeatability and good stability

Pending Publication Date: 2021-06-29
SUNSHINE LAKE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] For the drug dacomitinib, there are currently Chinese patent application CN107793368A disclosing four solvate crystal forms, but other more crystal forms and crystal forms with better performance / effect have not yet been discovered

Method used

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  • Novel crystal form of EGFR inhibitor, and preparation method thereof
  • Novel crystal form of EGFR inhibitor, and preparation method thereof
  • Novel crystal form of EGFR inhibitor, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] Embodiment 1: Preparation of crystal form N1

[0084] Weigh 200 mg of dacomitinib, suspend and stir in 10 mL of methanol at room temperature for 22 hours, filter and dry to obtain 162 mg of crystal form N1 product. After testing, its XRD pattern and figure 1 Basically the same.

Embodiment 2

[0085] Embodiment 2: the preparation of crystal form N2

[0086] Weigh 300 mg of dacomitinib, dissolve it in 5 mL of tetrahydrofuran, and slowly add 10 mL of n-propanol dropwise to precipitate a solid, then filter and dry to obtain 240 mg of crystal form N2 product. After testing, its XRD pattern and figure 2 Basically the same.

Embodiment 3

[0087] Embodiment 3: Preparation of crystal form N3

[0088] Weigh 200mg of dacomitinib, suspend and stir in 5mL of isopropanol at room temperature for 24h, filter and dry to obtain 156mg of crystal form N3 product. After testing, its XRD pattern and image 3 Basically the same.

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Abstract

The invention provides a novel crystal form of an EGFR inhibitor, and a preparation method thereof, and belongs to the field of medicinal chemistry. The crystal form has the characteristics of good stability and low toxicity. The preparation method comprises the following steps: suspending and stirring the EGFR inhibitor and a solvent, filtering, drying, and placing the dried product in humid air to obtain the product. The preparation method is simple to operate, mild in condition, good in crystallinity and easy for industrial production.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, in particular, the invention relates to a new crystal form of an EGFR inhibitor and a preparation method thereof. Background technique [0002] Dacomitinib is a second-generation irreversible EGFR inhibitor used for the first-line treatment of patients with EGFR mutations in NSCLC. Its chemical structure is as follows: [0003] [0004] Solid substances are formed by the accumulation of molecules. Due to the different ways of molecular accumulation, solid substances can be divided into crystalline substances and amorphous substances. In the molecules of crystalline substances, when one or several of the parameters such as unit cell parameters, molecular symmetry, analytical arrangement, molecular force, molecular conformation, crystal water and crystal solvent change, the existence of Two or more different crystal forms are called polymorphism. [0005] In drugs with polymorphic forms, the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12
CPCC07D401/12C07B2200/13
Inventor 徐巾超詹宁辛张杰叶辉青吴纯伟陈勇罗忠华
Owner SUNSHINE LAKE PHARM CO LTD
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