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Preparation method of demebeverine hydrochloride

A technology of norephrine and hydrochloride, which is applied in the preparation of organic compounds, chemical instruments and methods, preparation of aminohydroxyl compounds, etc., and can solve the problems of safety and high price

Inactive Publication Date: 2008-01-16
XINJIANG TECHN INST OF PHYSICS & CHEM CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] U.S. Patent US 3966813 reports a new synthetic method: using m-hydroxyacetophenone as raw material, reacting with tert-butyl nitrite to obtain oxime, and then obtaining norephrine hydrochloride through hydrogenation reduction, the total yield of the two-step reaction The rate is 70-80%, but tert-butyl nitrite has limited the application of this method in the synthesis of norfeline hydrochloride due to the high price, transportation and safety problems in use

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  • Preparation method of demebeverine hydrochloride
  • Preparation method of demebeverine hydrochloride
  • Preparation method of demebeverine hydrochloride

Examples

Experimental program
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Embodiment 1

[0014] Add 5ml of methanol to a 50ml single-necked bottle, add 0.75g of sodium metal after cooling to 0°C, stir until dissolved to obtain sodium methoxide, slowly add 10ml of nitromethane dropwise at 0°C, after dropping, stir at 0°C for 15 minutes to form Light yellow negative ion suspension, then dissolve 1.0g, 8.2mmol of m-hydroxybenzaldehyde in 10ml of nitromethane, slowly drop into the negative ion suspension, slowly rise to room temperature, stir overnight, add saturated ammonium chloride solution to terminate the reaction , the reaction solution was extracted with ethyl acetate, the organic phases were combined, washed with saturated brine, dried over anhydrous sodium sulfate, concentrated to obtain a light yellow oil, purified by column chromatography to obtain a light yellow solid intermediate 3-(1- Hydroxy-2-nitro)ethylphenol 1.104g, yield 73.6%, or 79.3% based on actual utilization of raw materials, and 72 mg of unreacted raw materials were recovered.

[0015] Add 20...

Embodiment 2

[0017] Add 10ml of nitromethane into a 50ml single-necked bottle, cool to 0°C, add 0.82g of solid potassium hydroxide 0.82g, 20.5mmol in batches, then add 2ml of anhydrous methanol, stir at 0°C for 60 minutes, and form a light yellow negative ion suspension solution, and then 1.0 g of m-hydroxybenzaldehyde, 8.2 mmol was dissolved in 10 ml of nitromethane, slowly added dropwise to the negative ion suspension, slowly raised to room temperature, stirred overnight, and saturated ammonium chloride solution was added to terminate the reaction, and ethyl acetate The reaction solution was extracted from the ester, the organic phases were combined, washed with saturated brine, dried over anhydrous sodium sulfate, and concentrated to obtain a brownish yellow oil, which was purified by column chromatography to obtain a light yellow solid intermediate product 3-(1-hydroxyl-2- Nitro)ethylphenol 1.06g, 70.1%, or 76.7% based on the actual raw material yield, and 80 mg of unreacted raw materia...

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Abstract

The present invention relates to a preparation method of norfenefrine hydrochloride. Said preparation method includes the following steps: using m-hydroxybenzaldehyde as raw material, using sodium methylate or potassium hydroxide as alkali, making them and nitromethane implement addition reaction, then making catalytic hydrogenation reaction to reduce nitro-group, finally making hydrochlorination so as to obtain the target compound.

Description

technical field [0001] The invention relates to a preparation method of drug norfeline hydrochloride. Background technique [0002] Norfenefrine hydrochloride, or Norfenefrine hydrochloride, scientific name m-hydroxyphenylethanolamine hydrochloride, English name Norfenefrine Hydrochloride, is an adrenaline-mimetic drug, which is a class of drugs that can excite nerves similar to epinephrine . There are two types of adrenergic receptors, α-receptors and β-receptors. α-receptors mainly exist on the effector cells of blood vessels such as glands, skin, mucous membranes and internal organs. When the α-receptor is excited, it mainly manifests as contraction of skin, mucous membrane blood vessels and visceral blood vessels, which increases peripheral resistance and blood pressure. Drugs that excite α-receptors are clinically used to increase blood pressure and resist shock. Norfeline hydrochloride is clinically used to excite α-receptors, constrict blood vessels, increase peri...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C213/00C07C213/02C07C215/60
Inventor 彭新湘杨建宏刘胜洋廖立新
Owner XINJIANG TECHN INST OF PHYSICS & CHEM CHINESE ACAD OF SCI