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A kind of istradefylline crude drug and preparation method thereof

A technology of istraphylline and a compound, applied in the field of istraphylline raw materials and preparation thereof, can solve the problems of not effectively reducing or avoiding the side effects of istraphylline and the like

Active Publication Date: 2020-05-05
JIANGSU HENGRUI MEDICINE CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, this product still contains the compound of formula III, and its quality control measures have not effectively reduced or avoided the side effects of istradefylline. Therefore, to improve the drug safety and effectiveness of istradefylline, and to better exert its clinical efficacy, It is very necessary to avoid or reduce its adverse reactions or side effects

Method used

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  • A kind of istradefylline crude drug and preparation method thereof
  • A kind of istradefylline crude drug and preparation method thereof
  • A kind of istradefylline crude drug and preparation method thereof

Examples

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specific Embodiment approach

[0057] The following examples are used to further describe the present invention, but these examples do not limit the scope of the present invention.

[0058] The experimental methods that do not specify specific conditions in the embodiments of the present invention usually follow conventional conditions or the conditions suggested by the raw material or commodity manufacturers. Reagents without specific sources are conventional reagents purchased on the market.

Embodiment 1

[0059] Example 1, EN-(6-amino-1,3-diethyl-2,4-dione-1,2,3,4-tetrahydropyrimidin-5-yl)-3-(3,4- Preparation of dimethoxy) propionamide (compound A)

[0060]

[0061] Suspend the compound of formula 1, 1,3-diethyl-5,6-diaminouracil (1.0kg, prepared according to EP0590919A1) in dichloromethane, add pyridine (1.6kg) under stirring, and dissolve in dichloromethane Compound 2 (1.54kg) in methane (3.5L) was added dropwise to the reaction system, and the addition was completed in about 1.5 hours. After stirring at room temperature for 15-20 hours, a saturated aqueous sodium bicarbonate solution was added dropwise to the reaction solution to adjust the pH to Around 7-8, a solid precipitated. After filtration, the filter cake was washed twice with water, and the filter cake was dried to obtain a pale yellow powdery solid product (1.56 kg) with a yield of 79.5%.

Embodiment 2

[0062] Example 2. Preparation of 8-((E)-2-(3,4-dimethoxyphenyl)vinyl)-1,3-diethyl-3,7-dihydro-1H-purine-2 Preparation of ,6-diketone (compound of formula I)

[0063]

[0064] Method A:

[0065] Add the compound of formula A (500g, 1.29mol) into a 10L reaction kettle, then add isopropanol (2.5L), stir, dissolve the solid sodium hydroxide (486g, 12.15mol) in water (2.0L), and then stir The reaction system was quickly added dropwise to the reaction system in about 30 minutes. The reaction was heated to 75-80°C. After 8-9 hours of reaction, TLC monitored the reaction of the raw materials. After the reaction was completed, the reaction solution was cooled to below 20°C, and then used 6M The pH of the reaction system was adjusted to 3-4 with hydrochloric acid, and a solid was precipitated. After filtering, the obtained filter cake was washed once with a small amount of water, and after drying, a light yellow-green powder product (383 g) was obtained with an HPLC purity of 99.34% and a ...

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PUM

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Abstract

The invention relates to an istradefylline raw material drug and a preparation method thereof. Specifically, the invention relates to an istradefylline raw material drug. A compound shown in formula III is not higher than 0.5% and is a medicine preparation consisting of the istradefylline raw material drug and a pharmacologically acceptable carrier and / or diluent. The raw material drug and the preparation thereof have better safety, effectiveness and stability. The formula III is shown in the description.

Description

Technical field [0001] The invention relates to a raw material medicine of istrafylline and a preparation method thereof. Background technique [0002] Itrafylline (Istradefylline, KW-6002, ) Is a non-dopamine compound oral adenosine A2a receptor antagonist developed by Kyowa Hakko Kirin, Japan. It improves the motor function of Parkinson's patients by changing the activity of neurons and can improve the early stage of Parkinson's patients. At the same time, it has brought a turning point in the treatment of patients with advanced Parkinson's, and proved to affect other neurotransmitters. Non-dopamine drugs can benefit patients with advanced Parkinson's; it and levodopa products (L-DOPA) Combined with Parkinson's disease patients to improve the symptoms of reduced efficacy, and can also reduce the dosage of levodopa, thereby preventing or delaying the occurrence of dyskinesia. [0003] In order to reduce or avoid the adverse effects of istrafylline, many domestic and foreign rese...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D473/06A61K31/522A61P25/14A61P25/16
CPCA61P25/14A61P25/16C07D473/06
Inventor 李长松南文汇孙绍光薛州洋
Owner JIANGSU HENGRUI MEDICINE CO LTD
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