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Application of phase transfer catalyst in synthesis of evogliptin

A catalyst and compound technology, applied in the field of drug synthesis, can solve the problems of low product yield, high cost, and poor quality, and achieve the effect of simple synthesis method, good product quality, and low cost

Inactive Publication Date: 2017-11-24
SUZHOU XINEN PHARMA
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  • 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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Experimental program
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Effect test

Embodiment

[0027] Preparation of compound (4)

[0028] At 0°C, add 20L of anhydrous dichloromethane, the reaction solvent, into a 50L reactor, then add 1.86 kg (10 mol) of compound (2), and then slowly add 1.24 kg (11 mol) of compound (3), keeping the temperature At around 0°C, after the addition was completed, TLC followed the reaction. After 6 hours, the reaction solution was added to 20L 5% sodium bicarbonate aqueous solution, separated, and the organic phase was concentrated under reduced pressure to obtain 2.47 kg (9.42 mol) of compound (4). ), the yield was 94.2%. HPLC detection purity: 98.1%.

[0029] 1 H NMR (400 MHz, CDCl 3 ) δ 6.53 (s, 1H), 5.47 (d, J = 12.5 Hz, 1H), 5.12 (t, J = 6.7 Hz, 1H), 4.32 (dt, J = 12.5, 5.3 Hz, 1H), 4.03 (d, J = 12.5Hz, 1H), 3.83 (dd, J = 12.4, 6.7 Hz, 1H), 3.67 (dt, J = 12.5, 5.3 Hz, 1H),3.62 – 3.45 (m, 2H), 3.38 (dt, J = 12.5, 5.3 Hz, 1H), 1.13 (s, 9H).

[0030] ESI+ [M+H] + =263.

[0031] Preparation of compound (6)

[0032] At ...

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Abstract

The present invention provides a method for synthesizing epigliptin, a compound of formula (1), which uses compounds of formula (2) and (3) as starting materials, and undergoes the following series of reactions to finally obtain the compound of formula (1), Namely the egagliptin: Compared with the prior art, there are many synthesis steps and complex synthesis process of egagliptin, but the synthesis method of the present invention is simple and easy, with low cost, high yield, good product quality, and is suitable for large-scale industrial production.

Description

technical field [0001] The invention relates to a method for synthesizing epagliptin, which belongs to the technical field of drug synthesis. Background technique [0002] Elogliptin (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 Elogliptin: 401.42; CAS registration number: 1222102-29-5; the structural formula is shown in Formula 1: [0003] [0004] Formula 1 [0005] Elogliptin was developed by Dong-A Pharmaceutical Company in South Korea. On October 2, 2015, it was approved by the Korean Ministry of Food and Drug Safety (MFDS) for the treatment of type 2 diabetes in South Korea. Ilogliptin is a DPP-4 inhibitor drug for the treatment of type 2 diabetes. Dosage specification: Elogliptin 5mg / tablet. [0006] prior art literature [0007] Non-patent literature: 1: Lab. Invest., 2016, 96, 5, P547-P560; Non-patent literature 2: ...

Claims

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Application Information

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IPC IPC(8): C07D241/08
CPCC07D241/08
Inventor 王保安
Owner SUZHOU XINEN PHARMA
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