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Preparation method of evogliptin

An equation and compound technology, applied in the field of organic chemical synthesis, can solve the problems of high cost, long synthetic route steps and high production cost, and achieve the effects of mild reaction conditions, low cost of raw materials and environmental friendliness.

Inactive Publication Date: 2017-06-20
上海倍殊生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0021] The steps of this synthetic route are long, and precious metal platinum is used, which is quite expensive and the production cost is high

Method used

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  • Preparation method of evogliptin
  • Preparation method of evogliptin
  • Preparation method of evogliptin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] The preparation of embodiment 1 formula I compound

[0060] Add 2,4,5-trifluorophenylacetic acid (38 g, 0.2 mol) into 1200 ml of dry tetrahydrofuran, start stirring, slowly add CDI (31 g, 0.22 mol), slightly exothermic, after the addition, add The reaction mixture was heated to 50°C. Isopropyl malonate (32 g, 0.22 mol) was added to the reaction system in batches, the reaction temperature was maintained at 50°C, and the addition was completed in about 30 minutes. After the addition, the reaction was continued for 4 hours. Concentrate the reaction solution under reduced pressure, pour the residue into a mixture of 200ml of water and 300ml of dichloroethane, adjust the pH to 2 with 0.1N dilute hydrochloric acid, separate the organic layer, and wash with 200ml of water and 200°C saturated brine in sequence The organic layer was dried over anhydrous magnesium sulfate, filtered and concentrated to obtain intermediate 1 (compound of formula I) as a white solid: 58.4 g, with a...

Embodiment 2

[0063] The preparation of embodiment 2 formula II compound

Embodiment 2-1

[0065] Intermediate 1 (compound of formula I) (31.6 grams, 0.1mol), compound of formula III (compound 3) (18.6 grams, 0.1mol), diisopropylethylamine (13.6 grams, 0.105mol) were added to 250ml of In isopropyl acetate, start stirring, heat up to 85°C, keep warm for 3 hours, cool down to room temperature, pour into 300ml of water, stir for 30 minutes, separate the organic phase, extract the aqueous phase with 200ml of isopropyl acetate once, combine The organic phase was successively washed with 300 ml of water and 300 ml of saturated brine, and dried over anhydrous magnesium sulfate. After filtration, the filtrate was concentrated under reduced pressure, and half of the isopropyl acetate was evaporated to obtain an isopropyl acetate solution of the compound of formula II (intermediate 2). Slowly drop 300ml of n-heptane into the isopropyl acetate solution, solids precipitate out, stir and crystallize at room temperature overnight, filter to obtain the compound of formula II (inte...

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Abstract

The invention relates to the field of organic chemical synthesis and in particular to a preparation method of evogliptin. Compared with an existing production line, the preparation method of evogliptin has the characteristics of being mild in reaction condition, low in cost of raw materials, environment-friendly and the like.

Description

technical field [0001] The invention relates to the field of organic chemical synthesis, in particular to a preparation method of egagliptin. Background technique [0002] Evogliptin was developed by Korea Dong-A Corporation and was approved for marketing by the Ministry of Food and Drug Safety (MFDS) of Korea on October 2, 2015. The trade name is Sugarnon. Evogliptin is a DPP-4 inhibitor used for type 2 diabetes. [0003] The structural formula of Evogliptin: [0004] [0005] In the prior art, the method for synthesizing epagliptin (Evogliptin) has: [0006] For example, [0007] (1) [0008] [0009] The synthesis route has long steps, high energy consumption at low temperature, sodium azide and potassium cyanide are highly toxic, and the cost is high and the environment is not friendly. [0010] (2) [0011] [0012] The synthesis route has long steps, high cost of raw materials, and high reaction energy consumption. [0013] (3) [0014] [0015] The...

Claims

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Application Information

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IPC IPC(8): C07D241/08
CPCC07D241/08
Inventor 王永刘利刚
Owner 上海倍殊生物科技有限公司
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