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Preparation method of compound containing 6-methyl uracil structure

A compound, dimethylformamide technology, applied in the field of preparation of compounds containing 6-methyluracil structure, can solve the problems of unfavorable industrial scale-up production, high price, low overall yield, etc., and achieve easy scale-up production and operation Simple, high reaction yield effect

Pending Publication Date: 2019-08-16
SUZHOU PENGXU PHARM TECH CO LTD +1
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] Based on the above reports, the existing schemes for the synthesis of compound 4 need to use expensive diketene or a large amount of other reagents to promote the reaction, and the overall yield is low, which is not conducive to industrial scale-up production

Method used

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  • Preparation method of compound containing 6-methyl uracil structure
  • Preparation method of compound containing 6-methyl uracil structure
  • Preparation method of compound containing 6-methyl uracil structure

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026]

[0027] Compound 1 (5.33 g), isopropanol (50 mL) and compound 2 (5 g) were added into a 100 mL three-neck flask, and the reaction was heated at 80-90 °C. After the reaction was completed, water (100 mL) was added and extracted with dichloromethane. The organic phases were combined, the solvent was removed by rotary evaporation, and 9.2 g of compound 3 was obtained by column purification, with a yield of 98% and a purity of 99.5%.

[0028] The NMR data of compound 3 are as follows:

[0029] 1 H NMR (400 MHz, DMSO) δ 12.91 (s, 1H), 11.66 (s, 1H), 7.73 (dd, J = 7.4,4.5 Hz, 3H), 4.94 (d, J = 5.0 Hz, 2H), 2.69 (s, 3H).

Embodiment 2

[0031] Add compound 1 and compound 2 into different reaction vials, and then add the following solvents respectively, heat the oil bath to 80-90 °C for 3 h, and take a sample for liquid chromatography. The liquid phase peak area test results of the product compound 3 are as follows.

[0032]

Embodiment 3

[0034]

[0035] Add compound 3 (5 g) and DMF (25 mL) into a 100 mL three-necked flask. Heating to 120~130 °C to react. After the reaction was completed, water (50 mL) was slowly added to precipitate a solid, which was filtered to obtain compound 4. Yield 82.5%, purity 98.0%.

[0036] The NMR data of compound 4 are as follows:

[0037] 1 H NMR (400 MHz, CDCl 3 ) δ 9.03 (s, 1H), 7.56 (d, J = 7.8 Hz, 1H), 7.46-7.41 (m, 1H), 7.30-7.25 (m, 1H), 5.61 (s, 1H), 5.38 (s, 2H), 2.17 (s, 3H).

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Abstract

The present invention relates to a preparation method and applications of a pharmaceutical intermediate 6-methyl uracil derivative, and a new compound involved in the preparation process of the pharmaceutical intermediate 6-methyl uracil derivative. Compared with the method in the prior art, the method of the present invention has characteristics of high reaction yield, good atomic economy, simpleoperation process, and easy production enlargement.

Description

technical field [0001] The invention relates to a preparation method and application of a pharmaceutical intermediate 6-methyluracil derivative. Background technique [0002] Endometriosis (EMS) refers to a common female gynecological disease caused by endometrial cells planted in abnormal positions, and is an estrogen-related disease. Endometrial cells should grow in the uterine cavity, but because the uterine cavity communicates with the ovaries and pelvic cavity through the fallopian tubes, endometrial cells can enter the ovaries, pelvic cavity and adjacent areas of the uterus for ectopic growth through the fallopian tubes. [0003] Studies have found that gonadotropin-releasing hormone (GnRH) agonists can reversibly shut down the pituitary signaling pathway after the initial stimulation, which can be used clinically to treat hormone-related diseases such as endometriosis and uterine fibroids. Some GnRH agonists based on this principle have been developed, but they have ...

Claims

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Application Information

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IPC IPC(8): C07D239/54C07D279/06
CPCC07D239/54C07D279/06C07B2200/09
Inventor 李丕旭王鹏谷向永杨海龙刘远华夏辉
Owner SUZHOU PENGXU PHARM TECH CO LTD
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