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

Asymmetric synthesis method of etglitin

A synthetic method and asymmetric technology, applied in the field of pharmaceutical synthesis, can solve the problems of low product yield, high cost, poor quality and the like, and achieve the effects of simple and easy synthesis method, good product quality and low cost

Inactive Publication Date: 2017-11-24
SUZHOU XINEN PHARMA
View PDF2 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] In the prior art, the synthesis process of epagliptin is often more complicated, the cost is higher, and there are also defects of low product yield and poor quality, which cannot be suitable for industrialized large-scale production

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0038] Preparation of compound (1)

[0039] Under the condition of 25℃, add the reaction solvent to the reaction kettle, then add the ammonia source, adjust the pH to 8.0 with hydrochloric acid, then add PLP (pyridoxal phosphate) and transaminase (G88L, I90E, G91Y, M124K), and slowly stir to Dissolve everything, then add compound (2) and react for 24 hours. After the reaction, adjust the pH to 2.0 with hydrochloric acid, add isopropyl acetate for extraction, leaving the aqueous phase, adjust the pH to 11.0 with aqueous sodium hydroxide, add isopropyl acetate After extraction, isopropyl acetate was concentrated under reduced pressure to obtain compound (1).

[0040] The reaction solvent is water and dimethyl sulfoxide, and the volume ratio of the two is 1:1.

[0041] The ammonia sources are isopropylamine and triethylamine, the concentration is 0.5M, and the molar ratio of the two is 1:1.

[0042] The mass concentration of the compound (2) is 100 g / L.

[0043] The mass concentration ra...

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 provides a synthesis method of a compound etglitin in a formula (1). A compound in a formula (2) is taken as a starting material, the compound, namely etglitin in the formula (1) is finally prepared through asymmetric catalytic reaction of transaminase. Compared with etglitin in the prior art, the etglitin provided by the invention is multiple in synthesis steps and complicated in synthesis process; the synthesis method is simple and feasible, relatively low in cost and relatively high in yield; the quality of a product is relatively good; and the synthesis method is suitable for industrial production.

Description

Technical field [0001] The invention relates to a method for synthesizing imagliptin and belongs to the technical field of drug synthesis. Background technique [0002] Itagliptin (generic name: EVOGLIPTIN, trade name Suganon), chemical name: (R)-4-((R)-3-amino-4-(2,4,5-trifluorophenyl)butyl Acyl)-3-(tert-butanol ether methyl)piperazin-2-one. The molecular weight of imagliptin: 401.42; CAS registration number: 1222102-29-5; the structural formula is shown in formula 1: [0003] [0004] Formula 1 [0005] Itagliptin was developed by South Korea's East Asia Pharmaceutical Company. It was approved by the Ministry of Food and Drug Safety (MFDS) in South Korea on October 2, 2015 for the treatment of type 2 diabetes. Imagliptin is a DPP-4 inhibitor drug used to treat type 2 diabetes. Dosage specification: Imagliptin 5mg / tablet. [0006] Prior art literature [0007] Non-Patent Literature: 1: Lab. Invest., 2016, 96, 5, P547-P560; Non-Patent Literature 2: BioorgMed Chem Lett, 2011, 21, 12...

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): C12P17/12C12N9/10
CPCC12P17/12C12N9/1096C12Y206/01
Inventor 王保安
Owner SUZHOU XINEN PHARMA
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