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Preparation method of trelagliptin succinate

A technology of trelagliptin succinate and drying is applied in the field of preparation of trelagliptin succinate, which can solve the problems of large use amount of drugs and long reaction time, and achieves the effect of speeding up the reaction time and saving materials

Inactive Publication Date: 2017-05-10
安徽省金楠医疗科技有限公司
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Problems solved by technology

[0002] According to the definition of drug in Article 102 of the "Drug Administration Law of the People's Republic of China", a drug refers to a drug that is used to prevent, treat, or diagnose human diseases, regulates human physiological functions purposefully, and specifies indications or functional indications. Substances, usage and dosage, including Chinese herbal medicines, Chinese herbal pieces, Chinese patent medicines, chemical raw materials and their preparations, antibiotics, biochemical drugs, radiopharmaceuticals, serum, vaccines, blood products and diagnostic drugs, etc., January 2013, National Development The National and Reform Commission issued a notice to decide to adjust the maximum retail price limit of respiratory, antipyretic and analgesic drugs and specialty special drugs from February 1, 2013, involving a total of 20 categories of drugs, more than 400 varieties, and more than 700 representative dosage forms Specifications, the average price reduction is 15%, and the average price reduction of high-priced drugs reaches 20%. Among them, trexagliptin succinate is an important drug. Disadvantages of high usage

Method used

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  • Preparation method of trelagliptin succinate

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Embodiment Construction

[0025] The embodiments of the present invention will be described in detail below with reference to the accompanying drawings, but the present invention can be implemented in many different ways defined and covered by the claims.

[0026] As shown in the accompanying drawing, the following steps are included:

[0027] Step 1: Mix 425g of 6-chloro-3-methyluracil, 714g of 2-cyano-5-fluorobenzyl bromide, 566ml of DIEA and 1530ml of NMP, heat up to 55℃~60℃ for reaction, add 2200ml of water to dilute and cool to about 5 °C, filtered, and the obtained solid was dried under reduced pressure at a temperature of 45 °C to 50 °C to obtain 697 g of compound C;

[0028] Step 2:

[0029] 1): Mix 684g of compound C, 441.8g of D hcl, 6150ml of isopropanol, 1420g of potassium carbonate and 45ml of water, stir the reaction at 55-60°C, monitor the reaction by TLC, add 2000ml of acetonitrile and cool to room temperature, stir After about 3 hours, filter, wash the filter cake twice with 2000ml o...

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Abstract

The invention discloses a preparation method of trelagliptin succinate. The preparation method comprises four steps. The method for preparing the trelagliptin succinate is rapid and efficient. By adopting the method disclosed by the invention, reaction time is shortened and materials are saved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical production methods, in particular to a preparation method of trexagliptin succinate. Background technique [0002] According to the definition of drug in Article 102 of the "Drug Administration Law of the People's Republic of China", a drug refers to a drug that is used to prevent, treat, or diagnose human diseases, regulates human physiological functions purposefully, and specifies indications or functional indications. Substances, usage and dosage, including Chinese herbal medicines, Chinese herbal pieces, Chinese patent medicines, chemical raw materials and their preparations, antibiotics, biochemical drugs, radiopharmaceuticals, serum, vaccines, blood products and diagnostic drugs, etc., January 2013, National Development The National and Reform Commission issued a notice to decide to adjust the maximum retail price limit of respiratory, antipyretic and analgesic drugs and specialty spe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/04
CPCC07D401/04
Inventor 胡惠平李杰卢海唐中姚
Owner 安徽省金楠医疗科技有限公司
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