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Preparation method of N-substituted phenyl glycine

A technology of phenylglycine and aniline, which is applied in the field of preparation of N-substituted phenylglycine (dabigatran etexilate intermediate), can solve the problems of poor purity, high cost, low yield, etc. The effect of high product purity and yield, and simple unit operation

Active Publication Date: 2014-08-20
ABA CHEM CORP
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Problems solved by technology

[0004] In this type of method, taking chloroacetic acid as the raw material product has poor purity and low yield
With bromoacetic acid as raw material, the cost is higher

Method used

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  • Preparation method of N-substituted phenyl glycine
  • Preparation method of N-substituted phenyl glycine
  • Preparation method of N-substituted phenyl glycine

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Embodiment Construction

[0022] The following are specific embodiments of the present invention, further describing the technical solution of the present invention, but the present invention is not limited to this embodiment.

[0023] (1) Synthesis of N-p-cyanophenylglycine (1)

[0024] In a 1000 mL hydrogenation reactor, add 45.9 g of 50% (w / w) glyoxylic acid aqueous solution, 500 ml of methanol, 0.5 g of palladium-carbon with 5% (w / w) palladium loading, and 35.4 g of 4-aminobenzonitrile, at room temperature (18~25°C) After stirring for 30 minutes, replace the system with hydrogen (referring to the gas in the reactor when feeding is air, at this time it is replaced with hydrogen, and the pressure is maintained at 10atm; this is a professional control process for production, and it cannot be added to 10atm at the beginning. , when the temperature rises, the pressure will rise, and the reaction will release heat at the same time, and the temperature will rise further. Generally, 2 to 3 atm hydrogen wil...

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Abstract

The invention discloses a preparation method of novel N-substituted phenyl glycine (dabigatran ester intermediate). The preparation method of the novel N-substituted phenyl glycine comprises the following processes: carrying out condensation on glyoxylic acid and cheap and available substituted phenylamine (1) which is taken as a starting raw material to obtain imide; meanwhile, carrying out hydrogenation reduction to obtain N-(substituted phenyl) glycine. The preparation method of the novel N-substituted phenyl glycine has the advantages that the synthetic route is not reported before, raw materials are cheap and easily available; unit operation is easy, and equipment requirement is low, so that the preparation method of the novel N-substituted phenyl glycine is applicable to industrial production.

Description

technical field [0001] The invention relates to a preparation method of N-substituted phenylglycine (dabigatran etexilate intermediate). Background technique [0002] N-substituted phenylglycine is an important intermediate of the new anticoagulant drug Dabigatran Etexilate developed and marketed by Boehringer Ingelheim, Germany. The synthesis method of its literature reports (WO2012009678, WO2009111997, CN1861596, US20050107355, etc.) is as follows : [0003] [0004] In this type of method, taking chloroacetic acid as the raw material product has poor purity and low yield. With bromoacetic acid as raw material, the cost is higher. Contents of the invention [0005] The technical problem to be solved by the present invention is to provide a new preparation method of N-substituted phenylglycine (dabigatran etexilate intermediate). [0006] The technical scheme that the present invention solves its technical problem to take is: [0007] A preparation method of N-subs...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C255/58C07C253/30C07D271/07
CPCC07D271/07C07C253/30C07C255/58
Inventor 林志刚刘艳琴徐军江岳恒蔡彤
Owner ABA CHEM CORP
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