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A kind of synthetic method of methyldopa

A synthesis method and technology of methyldopa, applied in chemical instruments and methods, preparation of organic compounds, organic chemistry, etc., can solve problems such as the influence of environment and operating conditions, and achieve low cost, high reaction yield and mild conditions. Effect

Active Publication Date: 2017-12-22
HUNAN XIANGYIKANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0012] The above-mentioned multiple reactions have their own advantages, but generally speaking, highly toxic cyanide is required in the reaction, which has a certain impact on the environment and operating conditions

Method used

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  • A kind of synthetic method of methyldopa

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Comparison scheme
Effect test

Embodiment 1

[0034] (A) Weigh 16.6g (0.1mol) of 3,4-dimethoxybenzaldehyde and 5.4g (0.1mol) of sodium methoxide into 150ml of dried dimethylformamide, stir to dissolve completely, and react Place the reactor in a cold water bath to control the temperature at about 20°C, weigh 14.5g (0.1mol) of methyl 2-acetamidopropionate, add it to the reactor in batches, stir the reaction, and complete the addition in at least 5 minutes. After all the addition was completed, the temperature was maintained and the reaction was stirred for 1.5h. After the reaction, add cold water to precipitate the intermediate, filter and wash the solid several times with cold water.

[0035] (B) Transfer the intermediate obtained in (A) to the reactor, add 150ml of dichloromethane to dissolve it, add 19.1g (0.1mol) of p-toluenesulfonyl chloride, 10.1g (0.1mol) of triethylamine ), after stirring and reacting for 2h, 4g of sodium borohydride was added, and the reaction was continued for 1h. After the reaction is finished...

Embodiment 2

[0039] (A) Weigh 166kg of 3,4-dimethoxybenzaldehyde and 54kg of sodium methoxide, put them into 500L of dried dimethylformamide, stir to dissolve completely, put the reactor in a cold water bath and control the temperature at 20 At about ℃, weigh 145 kg of methyl 2-acetylaminopropionate, add it into the reactor in batches, stir the reaction, and complete the addition in at least 5 minutes. After all the addition was completed, the temperature was maintained and the reaction was stirred for 2 h. After the reaction, add cold water to precipitate the intermediate, filter and wash the solid several times with cold water.

[0040] (B) Transfer the intermediate obtained in (A) to the reactor, add 500L of dichloromethane to dissolve it, add 191kg of p-toluenesulfonyl chloride and 101kg of triethylamine into the reactor, stir and react for 2.5h, then add boron Sodium hydride 4kg, continue to react for 1.3h. After the reaction is finished, add cold water and stir well, separate the l...

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Abstract

The invention discloses a method for synthesizing methyldopa, which specifically uses 3,4-dimethoxybenzaldehyde and 2-acetylaminopropionate methyl ester as raw materials to prepare the methyldopa after condensation, reduction, deprotection and purification. The synthesis route is simple, the yield is high, and the product purity is good.

Description

technical field [0001] The invention discloses a method for synthesizing methyldopa, which belongs to the field of organic synthesis. Background technique [0002] Levomethyldopa is an α2-receptor agonist cardiovascular drug. Its structural formula is as follows: [0003] . [0004] This product produces the metabolite α-methylnorepinephrine in the body, which blocks the central α receptor, thereby inhibiting the output of sympathetic impulses to the heart, kidney and peripheral blood vessels. At the same time, peripheral vascular resistance and plasma renal The activity of hormones is also reduced, thereby reducing blood pressure. This product can be used to treat high blood pressure, including high blood pressure in kidney disease. This product has high safety and is the drug of choice for the treatment of hypertension associated with pregnancy. [0005] In the prior art, the synthetic method of methyldopa has following several kinds: [0006] 1. Use veratrone as r...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C231/12C07C233/47C07C227/20C07C229/36C07C227/32
CPCY02P20/55
Inventor 帅放文王向峰章家伟
Owner HUNAN XIANGYIKANG PHARMA