Novel sunitinib salts and preparing method thereof

A technology for sunitinib and nisin salt compounds, applied in the field of new sunitinib salts and their preparation, to achieve the effects of good solubility and low thermal stability

Active Publication Date: 2014-07-02
SHANGHAI SYNCORES TECH INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] Patent WO 03 / 016305 discloses the preparation method of sunitinib malate, and screens other forms of salts (such as cyclamic acid, maleic acid, hydrobromic acid, mandelic acid, tartaric acid, fumaric acid, ascorbic acid , phosphoric acid, hydrochloric acid, p-toluenesulfonic acid, citric acid), screened by studying the properties related to the preparation of oral drugs such as crystallinity, stability, toxicity, hygroscopicity and morphology, but only sunitinib L- Preparation method of a salt of malic acid and two polymorphic forms thereof

Method used

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  • Novel sunitinib salts and preparing method thereof
  • Novel sunitinib salts and preparing method thereof
  • Novel sunitinib salts and preparing method thereof

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preparation example

[0048] In order to illustrate the present invention in more detail, the following preparation examples are given, but the scope of the present invention is not limited thereto.

[0049] The analytical detection condition of the present invention is as follows:

[0050] 1. DSC-TGA is measured by SDT Q600 of American TA Company, the test condition is 120ml / min N2, and the heating rate is 10℃ / min.

[0051] 2. X-ray powder diffraction data are measured by X′Pert Pro MPD (Multi-Purpose Diffractometer), light tube type: Empyrean XRD tube Cu LFF HR; voltage and current: 45 kV, 40 mA; goniometer: PW3050 / 60 vertical goniometer, radius 240mm; slit: DS=2°, SS=1 / 2°, mask=15mm, RS=5.0mm; detector: X′Celerator super energy detector; scanning mode: continuous scanning ; Scanning range: 3°-40°2θ; Counting time per step: 20s; Total scanning time: 6min.

Embodiment 1

[0052] Embodiment 1: sunitinib adipate

[0053] Mix 1.60 g of sunitinib and 0.60 g of adipic acid in pairs, add 60 ml of isopropanol and 6 ml of water, stir, heat to 50 ° C for 1 h to make the solution completely clear, continue to stir for 24 h, and the temperature drops to room temperature ( At about 25°C), crystals were precipitated, which were filtered by suction and washed with 10 ml of isopropanol to obtain 1.82 g of sunitinib adipate (form I).

Embodiment 2

[0054] Embodiment 2: sunitinib hemisuccinate

[0055] Mix 2.00 g of sunitinib and 0.40 g of succinic acid in pairs, add 40 ml of methanol and stir, heat to 50°C for 1 h to make the solution completely clear, then add 40 ml of ethyl acetate dropwise, continue stirring for 24 h, and the temperature drops to Crystals precipitated at room temperature (about 25°C), and were filtered with suction and washed with 10 ml of ethyl acetate to obtain 1.7 g of sunitinib hemisuccinate (form I).

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Abstract

The invention relates to novel medicinal sunitinib salts and a preparing method thereof. Sunitinib reacts with adipic acid, succinic acid, and pamoic acid in different solvent systems to respectively produce sunitinib adipate, sunitinib hemisuccinate, and sunitinib hemipamoate. The salts are both stable in the crystal form.

Description

technical field [0001] The invention mainly relates to a new pharmaceutically acceptable salt of sunitinib and a preparation method thereof. technical background [0002] Sunitinib is represented by formula (I) and its chemical name is N-[2-(diethylamino)ethyl]-5-[-(5-fluoro-1,2-dihydro-2-oxo- 3H-indole-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide, which is a novel multi-targeted tyrosine kinase inhibitor (TKI). [0003] [0004] WO 01 / 60814 mentioned many times the examples of salts of compounds of the general formula in the compound patents related to sunitinib and its derivatives, including quaternary ammonium hydrochloride, sulfate, malate, citrate, succinate acid salts, etc., but the nature of these salts and their preparation are not mentioned. [0005] Patent WO 03 / 016305 discloses the preparation method of sunitinib malate, and screens other forms of salts (such as cyclamic acid, maleic acid, hydrobromic acid, mandelic acid, tartaric acid, fumaric aci...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/06
CPCC07D403/06
Inventor 司永星方干王举波武文举张席妮
Owner SHANGHAI SYNCORES TECH INC
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