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Method for producing entacapone

A production method, entacapone technology, applied in the field of drug preparation, can solve problems such as poor product quality and complicated manufacturing process, and achieve the effects of low production cost, simple manufacturing process and high yield

Inactive Publication Date: 2015-07-01
李磊
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  • Application Information

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Problems solved by technology

Due to the current production process of entacapone, the manufacturing process is complicated and the product quality is poor

Method used

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Embodiment Construction

[0006] Now in conjunction with the present invention for further detailed description.

[0007] A kind of production method of entacapone of the present invention, specific steps are as follows: 1.83g3,4-dihydroxyl-5-nitrobenzaldehyde and 1.5gN,N-diethylcyanoacetamide and catalytic amount of piperazine Pyridyl acetate was dissolved in 40 mL of dry ethanol, stirred overnight to obtain 2.23 g of crude product; heated at 90 ° C, 3.0 kg of crude product was dissolved in 8.0 kg of acetic acid (or formic acid) containing 80 g of HBr (or 40 g of HCl), and slowly cooled to 20°C, and stirred at this temperature for 20h, then stirred at 15°C for 6h, filtered to collect the precipitated crystals, first carefully washed with a cold (4°C) 1L toluene-acetic acid (1:1 volume ratio) mixture, and then Wash with 1L of cold toluene and dry under vacuum at 45°C to obtain 2.4kg of crystalline pure entacapone.

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Abstract

The invention relates to a method for producing entacapone. The method comprises the following specific steps: dissolving 1.83g of 3,4-dihydroxy-5-nitrobenzaldehyde and 1.5g of N,N-diethyl cyanoacetamide and a catalytic amount of piperidine acetate in 40mL in dry ethanol, and stirring overnight to obtain 2.23g of a crude product; heating at 90 DEG, dissolving 3.0kg of the crude product in 8.0kg of acetic acid (or formic acid) containing 80g of HBr (or 40g of HCl), slowly cooling to 20 DEG C, and stirring at the temperature for 20 h, then stirring at 15 DEG C for 6 h, filtering, collecting precipitated crystal; and carefully washing the crystal with 1L of a cold mixed liquid (4 DEG C) of toluene-acetic acid (volume ratio of 1:1), then washing the crystal with 1L of cold toluene, and drying in vacuum at 45 DEG C to obtain 2.4kg of crystalline pure entacapone. The method for producing entacapone has the advantages of simple manufacture process, low production cost and high output.

Description

technical field [0001] The invention relates to the field of medicine preparation, in particular to a production method of entacapone. Background technique [0002] Entacapone belongs to catechol-O-methyltransferase (COMT) inhibitors, it is a reversible, specific COMT inhibitor that mainly acts on the periphery, and it is used simultaneously with levodopa preparations. This product reduces the metabolism of levodopa to 3-oxo-methyldopa (3-OMD) by inhibiting the COMT enzyme, which increases the bioavailability of levodopa and increases the total amount of levodopa available in the brain. This effect has been confirmed in clinical trials. Due to the current production process of entacapone, the manufacturing process is complicated and the product quality is poor. Contents of the invention [0003] The technical problem to be solved by the present invention is: in order to overcome the above-mentioned problems, a production method of entacapone is provided. [0004] The te...

Claims

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Application Information

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IPC IPC(8): C07C255/41C07C253/30
Inventor 李磊
Owner 李磊
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