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A kind of preparation method of sitagliptin impurity

A sitagliptin impurity and addition reaction technology, applied in the field of preparation of sitagliptin impurities, can solve the problems of poor qualitative and quantitative accuracy, no reference substance, supply, etc., achieve low production cost and improve accuracy , the effect of low energy consumption

Active Publication Date: 2019-09-13
HEFEI HUAFANG PHARMA SCI & TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Impurity Ⅰ is recorded in the European Pharmacopoeia and the USP sitagliptin standards, but there is no supply of reference substances, and there is no report on the synthesis method of this impurity in domestic and foreign literature and patents. Currently, the self-control method is used, and the accuracy of its qualitative and quantitative Inadequate, in order to improve the quality of sitagliptin phosphate tablets and sitagliptin metformin tablets and reduce the risk of clinical use, it is necessary to study and monitor the impurities in sitagliptin phosphate tablets and sitagliptin metformin tablets

Method used

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  • A kind of preparation method of sitagliptin impurity
  • A kind of preparation method of sitagliptin impurity
  • A kind of preparation method of sitagliptin impurity

Examples

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Embodiment 1

[0034] Mix sitagliptin, fumaric acid, pyridine, and tetrahydrofuran, heat up to 40°C, keep stirring for 15 hours, concentrate under reduced pressure, add ethanol to mix, filter the filtrate, crystallize at low temperature, and dry to obtain the sitagliptin impurity , wherein the molar ratio of sitagliptin to fumaric acid is 1:1, and the weight ratio of pyridine to sitagliptin is 3:50.

Embodiment 2

[0036] Mix sitagliptin, fumaric acid, triethylamine, and N,N-dimethylformamide, raise the temperature to 70°C, keep stirring for 4 hours, concentrate under reduced pressure, add ethanol to mix, filter the filtrate, and analyze at low temperature crystallized and dried to obtain sitagliptin impurities, wherein the molar ratio of sitagliptin to fumaric acid was 1:1.2, and the weight ratio of triethylamine to sitagliptin was 2:50.

Embodiment 3

[0038] Sitagliptin, fumaric acid, AlCl 3 , tetrahydrofuran, mixed evenly, heated to 55°C, kept stirring for 12h, concentrated under reduced pressure, mixed with ethanol, filtered to take the filtrate, crystallized at low temperature, and dried to obtain sitagliptin impurities, wherein sitagliptin and fumaric acid The molar ratio is 1:1.12, AlCl 3 The weight ratio of sitagliptin and sitagliptin is 1.1:20.

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Abstract

The invention discloses a preparation method of sitagliptin impurities. The preparation method comprises the following steps: taking sitagliptin and fumaric acid as raw materials and carrying out addition reaction under the action of a catalyst to prepare the sitagliptin impurities. The preparation method has the advantages of short reaction route, low energy consumption, low production cost and simplicity for operation and is suitable for industrial production; the preparation method has high yield and the purity of the prepared sitagliptin impurities is high.

Description

technical field [0001] The invention relates to the technical field of chemical substance preparation, in particular to a method for preparing sitagliptin impurities. Background technique [0002] According to the data and estimates of diabetes and impaired glucose tolerance (IGT) released by the International Diabetes Federation (IDF), the number of diabetic patients in 2003 was 194 million, and it will reach 333 million in 2025; It will be as high as 472 million. In recent years, with the continuous improvement of people's living standards and changes in dietary structure, the number of diabetic patients in my country has also experienced a large-scale increase. [0003] The anti-diabetic drugs currently in clinical use mainly include insulin, sulfonylurea, metformin, and recently listed α-glucosidase inhibitors and insulin sensitizers such as thiazolidinedione drugs. These drugs have a good curative effect, but there are still disadvantages that the long-term use of the...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/04
Inventor 高永好陈仕云何勇彭扶云吴宗好
Owner HEFEI HUAFANG PHARMA SCI & TECH
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