A kind of preparation method of S-glycidyl phthalimide

A technology of glycerol phthalimide and potassium phthalimide, applied in the direction of organic chemistry and the like, can solve the problems of increased risk factor, unsuitable for industrial production and the like

Active Publication Date: 2016-04-20
CHENGDU GUOHONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since the microwave reaction is a closed system reaction, it has certain risks and is only suitable for a small amount of laboratory synthesis. After the scale-up production, the risk factor will increase greatly, and it is not suitable for industrial production.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Add 85g (0.46mol) of potassium phthalimide, 10.5g (0.046mol) of benzyltriethylammonium chloride, 0.76g (0.0046mol) of potassium iodide, and 382.5ml of isopropanol into a 1L single-necked bottle, and stir Evenly, add (S) epichlorohydrin 85.6g (0.93mol) to the reaction system under stirring at 28°C, the system changes from white turbidity to light yellow turbidity, and react at 28°C for 72 hours, Suction filtration, washing with water, and drying to finally obtain 88.1 g of solid, with a yield of 94.5% and a purity of 92%.

Embodiment 2

[0037] Add 85g (0.46mol) of potassium phthalimide, 10.5g (0.046mol) of benzyltriethylammonium chloride, 0.76g (0.0046mol) of potassium iodide, and 382.5ml of isopropanol into a 1L single-necked bottle, and stir Evenly, add (S) epichlorohydrin 85.6g (0.93mol) to the reaction system under stirring at 32°C, the system changes from white turbidity to light yellow turbidity, and react at 32°C for 72 hours, Suction filtration, washing with water, and drying to finally obtain 87.7 g of solid, with a yield of 94.0% and a purity of 90%.

Embodiment 3

[0039] Add 85g (0.46mol) of potassium phthalimide, 10.5g (0.046mol) of benzyltriethylammonium chloride, 0.76g (0.0046mol) of potassium iodide, and 850ml of isopropanol into a 1L single-necked bottle, and stir well , at 30°C, add 85.6g (0.93mol) of (S) epichlorohydrin to the reaction system while stirring, the system changes from white turbidity to light yellow turbidity, react at 30°C for 110 hours, pump Filter, wash with water, and dry to finally obtain 85.4 g of solid, with a yield of 91.5% and a purity of 89%.

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PUM

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Abstract

The invention relates to a reaction of potassium phthalimide or phthalimide and (S) epichlorohydrin, adding a phase transfer catalyst and potassium iodide to synthesize S-glycidyl phthalate A new approach to formimides. Compared with the prior art, the synthesis method can greatly improve the yield of the obtained S-glycidyl phthalimide product, and the operation is simple, the technological process is simple and safe, the product has high purity and low cost, and is extremely suitable for industrial production of S-glycidyl phthalimide. - Glycidylphthalimide.

Description

technical field [0001] The invention relates to the field of chemical synthesis, in particular to a preparation method of S-glycidyl phthalimide. Background technique [0002] S-glycidyl phthalimide is an important intermediate for the preparation of oxazolidinone compounds such as the new antibiotic linezolid and the new oral anticoagulant drug rivaroxaban, and it is also the preparation of antifungal thiooxazolidine Ketones, oxazolidinedione, amide compounds used as growth hormone secretagogues, important intermediates of heterocyclic compounds such as morpholino urea derivatives used to treat inflammation. [0003] The preparation method of S-glycidyl phthalimide is usually synthesized by the method described in TetrahedronAsym.1996,7,1641 by A.Gutcait et al. The method is based on phthalimide and (S) epichlorohydrin as raw materials, in diethyl azodicarboxylate (DEAD) and triphenylphosphine (PH 3 In the presence of P), tetrahydrofuran was used as a solvent and reacted ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D405/06C07D263/20C07D413/14
Inventor 武永财郭晖郭礼新
Owner CHENGDU GUOHONG PHARMA
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