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Method for synthesizing carbidopa

A synthetic method, the technology of oxyaziridine, applied in hydrazine preparation, organic chemistry, etc., can solve the problems of unsuitable carcinogenic effect of cyclohexanone, unqualified product residue, inconvenient recovery and application, etc., and achieve good product quality and high yield high effect

Active Publication Date: 2014-05-14
SHANDONG XINHUA PHARMA CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But there are also two deficiencies: 1. cyclohexanone is used in the preparation of 3,3-pentamethyleneoxyacridine in the process as a raw material. On the one hand, cyclohexanone has carcinogenic effect and should not be used for drug synthesis; on the other hand, cyclohexanone Ketone has a high boiling point (155.6°C), which is not convenient for recycling and may easily cause unqualified residues in the product

Method used

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  • Method for synthesizing carbidopa
  • Method for synthesizing carbidopa
  • Method for synthesizing carbidopa

Examples

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Embodiment 1

[0029] (1) Preparation of Oxyaziridine

[0030] Add 0.044mol chloramine to 100ml of 1N NaOH solution under stirring to form a solution, then drop it into 100ml of dichloromethane solution containing 10ml of acetone under vigorous stirring, and control the temperature at 20°C. After adding, stir for 30 seconds and stop Stir and remove the aqueous layer. The dichloromethane layer contained 3,3-dimethyloxyaziridine in a theoretical amount of 43.5%. Dry the organic layer with anhydrous sodium sulfate, control the reflux ratio of 1:3 and concentrate with a fractionation column until the content of oxyaziridine is 0.9 mol / L.

[0031] (2) Preparation of imidate

[0032] With the dichloromethane solution of 0.073mol above-mentioned oxaziridine, control temperature is 25 ℃, drop in the 50ml dichloromethane liquid of the methyl dopa methyl ester of 0.068mol in 15~20 minutes, dripping finishes, in Stir at this temperature, cool down to 0°C, and filter to obtain methyl dopamine ester. ...

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Abstract

The invention belongs to the field of chemical synthesis, and in particular relates to a method for synthesizing carbidopa. The method is characterized by comprising the following steps of: reacting oxaziridine with methyldopa ester to obtain methyldopa imido ester, and hydrolyzing to obtain the carbidopa. The method has the advantages that the carbidopa is prepared by a brand-new process, the used raw materials are favorable for synthesizing a medicine, and the prepared carbidopa is high in yield and quality.

Description

technical field [0001] The invention belongs to the field of chemical synthesis, in particular to a synthesis method of carbidopa. Background technique [0002] Carbidopa, English name: Carbidopa, is (S)-α-methyl-α-hydrazino-3,4-dihydroxyphenylpropionic acid monohydrate, carbidopa has a strong peripheral dopa decarboxylation Enzyme inhibitors. It is not easy to pass through the blood-brain barrier. When used in combination with levodopa, it only inhibits the activity of peripheral dopa decarboxylase, reduces the generation of dopamine in peripheral tissues, and reduces its peripheral adverse reactions, thereby increasing the amount of levodopa entering the central nervous system and improving brain function. The concentration of dopamine in the body enhances the curative effect of levodopa, so it is an important adjuvant drug of levodopa. Carbidopa alone is ineffective. In clinical practice, carbidopa and levodopa are usually combined in a ratio of 1:10 or 1:4 to make a co...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C243/18C07C241/02
Inventor 李兴泰黄爱军宋丽华易晓清赵丽李敏之
Owner SHANDONG XINHUA PHARMA CO LTD
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