Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

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
View PDF9 Cites 8 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Preparation method for saxagliptin
  • Preparation method for saxagliptin
  • Preparation method for saxagliptin

Examples

Experimental program
Comparison scheme
Effect test

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...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com