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Neratinib compound

A technology of neratinib and its compounds, which is applied in the field of neratinib compounds and their preparation, can solve problems such as poor method reproducibility, high impurity content, content and crystal form cannot be reproduced, and achieve good stability and high The effect of purity

Inactive Publication Date: 2018-03-09
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] There are multiple preparation methods for neratinib, among which the preparation method of neratinib is disclosed in U.S. Patent No. 7,399,865, but no matter what method, the purity of neratinib obtained is low and the impurity content is high; the method reproducibility is poor , it is difficult to scale up to the pilot scale, so that the content and crystal form cannot be reproduced

Method used

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  • Neratinib compound
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Experimental program
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Embodiment 1

[0030] In a 50L reactor, add 3 kg of neratinib (purity 97.3%, HPLC) and 30.3 L of water-acetone-ammonia=9:0.8:1.1 mixture, heat to 88°C-91°C, add 150 gram of activated carbon, insulated and stirred for 30 minutes, filtered while hot, and the filtrate was naturally cooled to room temperature under stirring, and then incubated for 5.5 hours, crystallization was precipitated, filtered, and vacuum-dried at room temperature to obtain 2.81 kilograms of neratinib crystals. Melting point: 198.5°C-199.6°C, purity 99.95%, single impurity 0.04%, MS: 349.13 (M+H) solvent residue detection meets the requirements.

[0031] The X-ray instrument model and measurement conditions of the crystal: Rigaku D / max 2500 diffractometer; CuKa 40Kv100mA; 2θ scanning range: 0-50 ° .

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Abstract

The invention belongs to the technical field of medicine, and specifically relates to neratinib and a preparation method thereof. The new crystal form of neratinib obtained in the invention has the advantages of high purity, the largest impurity is less than 0.5‰, good stability, and heavy method. The reproducibility is good, and the purity and crystal form can be well reproduced when it is scaled up to the pilot scale.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a neratinib compound and a preparation method thereof. Background technique [0002] Neratinib (neratinib, HKI-272) is an oral irreversible pan-ErbB receptor tyrosine kinase inhibitor that is currently undergoing phase III clinical trials worldwide by Pfizer, which can effectively inhibit ErbB1 and ErbB2 tyrosine Kinase activity, the mechanism of its action is to inhibit the ATP sites of EGFR (ErbB-1) and HER2 (ErbB-2) in cells to prevent phosphorylation and activation of tumor cells, through EGFR (ErbB-1) and HER2 (ErbB-2) ) homogeneous and heterogeneous dimers block the down-regulation signal, so as to achieve the purpose of tumor control. For patients with ErbB-2-positive advanced breast cancer, oral neratinib has shown good clinical effects. [0003] The structural formula of neratinib is as follows: [0004] [0005] Chemical name: (2E)-N-[4-[[3-chloropyri...

Claims

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Application Information

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IPC IPC(8): C07D401/12A61K31/4709A61P35/00
CPCC07D401/12C07B2200/13
Inventor 严洁王志凤
Owner TIANJIN HANKANG PHARMA BIOTECH
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