Preparation method for saxagliptin

A compound and dropping technology, applied in the preparation of sulfonamides, organic chemistry, etc., can solve the problems of difficult preparation and storage of biological enzymes, and achieve the effects of solving difficult preparation and storage, reducing production costs, and high yield

Inactive Publication Date: 2014-10-15
天津民祥生物医药股份有限公司
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  • Claims
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AI Technical Summary

Problems solved by technology

[0008] In the prior art, compounds 5 to 6 have to be split by biological enzymes. Since biological enzymes are not easy to prepare and store, it is necessary to seek an alternative method for the preparation of saxagliptin

Method used

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  • Preparation method for saxagliptin
  • Preparation method for saxagliptin
  • Preparation method for saxagliptin

Examples

Experimental program
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Embodiment

[0034] A preparation method of saxagliptin, compound 5 [2-(3-hydroxy-1-adamantyl)-2-1-oxoacetic acid (3)] to compound 7 (N-tert Butoxycarbonyl-3-hydroxyl-1-adamantylglycine) is carried out by replacing the reaction process of compound A to G in the following steps:

[0035](1) Put 130ml of absolute ethanol into a three-necked flask, cool it in an ice-salt bath to below -5°C, slowly add thionyl chloride (8ml, 110mmol) dropwise, and control the temperature not to exceed -5°C during the dropwise addition; After the addition was completed, compound A (20 g, 89 mmol) was added in batches, and the temperature was controlled to be lower than -5°C during the addition; after the addition was completed, the reaction solution was stirred at room temperature for 5 h, then the reaction solution was concentrated to 50 ml, and cooled to Below 0°C, add 100ml of toluene and 20g of triethylamine respectively; the reaction solution is stirred at 0°C for 30 minutes and then filtered, the filter c...

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Abstract

The invention discloses a preparation method for saxagliptin. The preparation method for the saxagliptin uses a chemical synthesis method to replace saxagliptin intermediate preparation in a traditional technique and uses chiral inducer in the reaction to perform chiral synthesis. The preparatoin method for the saxagliptin is easy and convenient to operate, is high in yield, enables the intermediate production cost to be lowered and solves the technical problem of difficulty in biological enzyme preparing and storing due to the fact that the traditional technique needs to use biological enzyme to perform resolution.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to a preparation method of saxagliptin. Background technique [0002] Saxagliptin, an incretin-based hypoglycemic drug jointly developed by two global pharmaceutical companies, Bristol-Myers Squibb and AstraZeneca, has been launched in many countries including the United States, India and the European Union. 46 countries within the country have obtained marketing approval. Saxagliptin, a potent dipeptidyl peptidase-4 inhibitor, is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes. [0003] In May 2011, it was officially approved by SFDA in China. The drug can be used as a monotherapy, or in combination with metformin on the basis of poor control of metformin. Clinical studies have confirmed that saxagliptin has the advantages of outstanding curative effect and long-lasting effect. [0004] The chemical structure of saxaglipt...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D209/52C07C311/06C07C303/40
CPCC07D209/52
Inventor 张杰刘万里薛志杰曹晖李金娜陈瑞香宋建民
Owner 天津民祥生物医药股份有限公司
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