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
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  • 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

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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...

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PUM

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Abstract

The present invention provides a method for synthesizing igliptin, a compound of formula (1). The compound of formula (2) is used as a starting material, and the compound of formula (1) is finally prepared through asymmetric catalytic reaction of transaminase. Ilogliptin: Compared with the prior art, the edagliptin has many synthesis steps and complicated synthesis process, and the synthesis method of the present invention is simple and easy to implement, has lower cost, higher yield and better product quality, and is suitable for large-scale 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

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12P17/12C12N9/10
CPCC12P17/12C12N9/1096C12Y206/01
Inventor 王保安
Owner SUZHOU XINEN PHARMA
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