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A kind of preparation method and intermediate of pyrimidone heteroaryl derivatives

一种化合物、立体异构体的技术，应用在嘧啶酮并杂芳基类衍生物的制备领域，能够解决不利工业扩大生产、批量小、产率低等问题

Active Publication Date: 2021-11-12
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] This method has problems such as small batch size, thin-layer chromatography purification and low yield in the post-processing method, wherein the reaction yield of compound 9d is 69%, and the yield of product 11 in the last step is only 24.7%, which is not conducive to industry Expand production; and, adding hydrochloric acid in the aftertreatment of preparation 9e, causes the generation of chlorinated impurity, and this impurity is difficult to remove, and it is necessary to improve its preparation method

Method used

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  • A kind of preparation method and intermediate of pyrimidone heteroaryl derivatives
  • A kind of preparation method and intermediate of pyrimidone heteroaryl derivatives
  • A kind of preparation method and intermediate of pyrimidone heteroaryl derivatives

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specific Embodiment approach

[0115] The following examples are used to further describe the present invention, but these examples do not limit the scope of the present invention.

[0116] The experimental methods not indicating specific conditions in the examples of the present invention are generally in accordance with conventional conditions, or in accordance with the conditions suggested by raw material or commodity manufacturers. Reagents without specific sources indicated are conventional reagents purchased in the market.

Embodiment 1

[0121] Example 1, 1-(4-(7-(2,6-difluorobenzyl)-3-((dimethylamino)methyl-5-(6-methoxypyridazin-3-yl)- Preparation of 4,6-dioxo-4,5,6,7-tetrahydro-2H-pyrazol[3,4-d]pyrimidin-2-yl)phenyl)-3-methoxyurea

[0122]

[0123] The first step, preparation of formula (VI-1-1) compound

[0124]Suspend raw material VII-1 (90g) in methanol (900mL), add 30% sodium methoxide methanol solution (101g), stir and react in an oil bath at 30°C for about 15 hours, after the reaction, add isopropanol (1.8L) , stirred evenly, cooled to room temperature and then frozen and crystallized for 4h; filtered, collected the filter cake, and slurried with acetone (320mL) for 1.5 hours, cooled in an ice bath, filtered, collected the filter cake, and dried in vacuo to obtain the title product (65.9g). The yield is 81.0%, and the purity is 99.27%.

[0125] Second step, preparation of formula (IV-1) compound

[0126] Add raw material VI-1-1 (1100g), N,N-dimethylformamide (7.0kg) into the reaction flask, stir ...

Embodiment 2

[0135] Example 2, the preparation of compound 1-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6- Methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-3- Methoxyurea (shown in formula (I-2))

[0136]

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Abstract

The invention relates to a preparation method of pyrimidone heteroaryl derivatives and an intermediate thereof. Specifically, the present invention prepares pyrimidone heteroaryl derivatives by changing starting materials and intermediates. The method shortens the reaction steps, improves the reaction yield, is simple and easy to operate, and is beneficial to industrial expansion production.

Description

technical field [0001] The invention relates to a preparation method of pyrimidone heteroaryl derivatives and an intermediate thereof. Background technique [0002] Endometriosis is a common estrogen-dependent gynecological disease that often occurs during women's reproductive years, and its mechanism of action is still unclear. The difficult diagnosis of endometriosis and the complex symptoms of unknown etiology have seriously hindered the discovery of effective treatments. At present, endometriosis is mainly diagnosed by laparoscopy and treated by surgery, or taking contraceptives, GnRH receptor agonists or progestins to reduce estrogen levels in the body to control. [0003] Gonadotropin-releasing hormone (Gonadoliberin; gonadotropin releasing hormone; GnRH), also known as luteinizing hormone-releasing hormone (LHRH), is a decapeptide hormone (pGlu-His-Trp-Ser-Tyr-Gly- Leu-Arg-Pro-Gly-NH2), is a central regulator in the endocrine reproductive system. It is transported ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/04A61K31/519A61P35/00A61P15/00
CPCA61P15/00A61P35/00C07D487/04C07D495/04A61K31/519A61P15/02C07D513/04C07D471/04
Inventor 贾君磊刘兵高晓晖
Owner JIANGSU HENGRUI MEDICINE CO LTD
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