Preparation method of compound containing 6-methyluracil structure

The technology of a compound and an organic solvent is applied in the field of preparation of compounds containing 6-methyluracil structure, can solve the problems of hot flash-related bone mineral density, delayed onset of action, side effects, etc., and achieves strong impurity removal ability and simple post-processing , the effect of high reaction yield

Inactive Publication Date: 2019-06-11
SUZHOU PENGXU PHARM TECH CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Some GnRH agonists based on this principle have been developed, but they have certain limitations, such as the need for injection to have a therapeutic effect, the onset of action is delayed, and side effects often occur, such as hot flashes and decreased bone density

Method used

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  • Preparation method of compound containing 6-methyluracil structure
  • Preparation method of compound containing 6-methyluracil structure
  • Preparation method of compound containing 6-methyluracil structure

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025]

[0026] Add 1.0 g of compound 2 and 1.07 g of compound 1 into the reaction flask, add 5 mL of DMF, heat up to 140 °C and stir for 0.5 h, HPLC monitors that the conversion of the raw materials is complete, cool down to room temperature, add 15 mL of water to quench the reaction, and a large amount of Solid, stirred for 0.5h, filtered to obtain the crude product, directly added the crude product to 1 mL of ethanol, heated to 80-90°C, continued to stir for 1h, then slowly cooled to 5-10°C, filtered, and drenched with 0.5ml of ethanol Washing, the product was a white solid with a yield of 67% and a purity of 98.6%.

[0027] The NMR data of compound 3 are as follows:

[0028] 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).

[0029] M+H molecular ion peak 303.1.

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Abstract

The invention relates to a preparation method and application of a medical intermediate 6-methyluracil derivative. Compared with the prior art, the method disclosed by the invention for synthesizing medical active molecules has the following advantages of good atom economy, high reaction yield, simple post-treatment and high impurity removal capability, and the obtained product has high purity.

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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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/54
Inventor 李丕旭王鹏杨海龙刘远华夏辉
Owner SUZHOU PENGXU PHARM TECH CO LTD
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