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Sitagliptin impurity, and preparation method and detection method thereof

A kind of technology of sitagliptin and detection method

Inactive Publication Date: 2021-10-01
ZHEJIANG MENOVO PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] However, in the process of drug development, we found a new impurity with a new structure, and the content of this new impurity in the product was above 0.1%, which affected the purity and yield of sitagliptin

Method used

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  • Sitagliptin impurity, and preparation method and detection method thereof
  • Sitagliptin impurity, and preparation method and detection method thereof
  • Sitagliptin impurity, and preparation method and detection method thereof

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Embodiment Construction

[0043] The present invention will be further described in detail below in conjunction with the accompanying drawings and embodiments.

[0044] The sitagliptin impurity of the present invention is that the sitagliptin impurity is (R)-3-amino-N'-(2-(3-(trifluoromethyl)-5,6-dihydro-[1,2 ,4] Triazolo[4,3-a]pyrazin-7(8H)-yl)acetyl)-4-(2,4,5-trifluorophenyl)butanohydrazide, whose structural formula is:

[0045]

[0046] In the present embodiment, the preparation method of above-mentioned sitagliptin impurity is:

[0047] In the solution that 19g hydrazine hydrate is dissolved in 2000ml isopropanol, at 0-5 ℃, add di-tert-butyl dicarbonate solution (50g di-tert-butyl dicarbonate is dissolved in 250ml isopropanol), react The material was stirred at room temperature until the reaction was monitored by TLC. After the reaction was completed, the reaction material was distilled under vacuum to obtain the product of formula III, which was dissolved in 1000 ml of tetrahydrofuran and cool...

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Abstract

The invention relates to a sitagliptin impurity, and a preparation method and a detection method thereof. The new impurity found by the invention can provide standard reference for quality control of sitagliptin and safety detection of clinical medication, so that the safety and reliability of clinical medication are ensured. Besides, the preparation method of the impurity compound provided by the invention is simple to operate and mild in reaction condition, the impurity compound with high purity and high yield can be obtained, and the preparation method is used for further researching the property of the impurity and providing technical support for controlling the content of the sitagliptin compound and solving the problems of impurity limit of sitagliptin and safety of related products; and the detection method of the sitagliptin impurity can carry out targeted qualitative detection on the impurity, is high in detection precision, and is beneficial to providing a technical means for detection of the impurity in the sitagliptin, so that the quality of the sitagliptin is controlled.

Description

technical field [0001] The invention relates to a sitagliptin impurity, a preparation method and a detection method thereof. Background technique [0002] Sitagliptin is an oral dipeptidyl peptidase-4 (DPP-4) inhibitor used in combination with diet and exercise to improve glycemic control in patients with type 2 diabetes. The action of this drug results in a glucose-dependent increase in insulin and a decrease in glucagon to improve blood sugar control. Sitagliptin was approved by the FDA on October 16, 2006. Sitagliptin Phosphate Monohydrate——(3R)-3-Amino-1-[3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,2,4-triazolo The chemical formula of [4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one dihydrogen phosphate monohydrate is as follows: [0003] [0004] Sitagliptin impurities listed in the European Pharmacopoeia and the USP are as follows: [0005] [0006] However, in the process of drug development, we found a new impurity with a new structure, and the conten...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04G01N30/02G01N30/06G01N30/36
CPCC07D487/04G01N30/02G01N30/06G01N30/36Y02P20/55
Inventor 塔内加·阿米特·库玛普拉萨德·达南库拉黄想亮黄勤钟泽华
Owner ZHEJIANG MENOVO PHARMA
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