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Synthesis method of budesonide impurity EP-ZG

A technology of EP-ZG and synthesis method, which is applied in the field of drug impurity synthesis to achieve the effects of high yield, good selectivity and simple process route

Inactive Publication Date: 2019-08-09
BIONNA (BEIJING) MEDICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently, there is no synthetic method specifically for budesonide impurity EP-ZG in the prior art

Method used

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  • Synthesis method of budesonide impurity EP-ZG
  • Synthesis method of budesonide impurity EP-ZG
  • Synthesis method of budesonide impurity EP-ZG

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018]

[0019] Take a 1000mL three-neck flask, add 3.01g of budesonide and 900mL of ethanol, stir to dissolve; then add 1.10g of triphenylphosphine rhodium chloride, the system changes from colorless and clear to reddish brown, and hydrogen gas is introduced into the solution and replaced three times. Carry out the reaction at room temperature until the liquid phase detection shows that there is no residue of the raw material budesonide; then directly filter the system, concentrate and dry the filtrate to obtain a black oil, and separate the black oil by column chromatography to obtain 2.7g of gray-brown foamy solid ; The obtained gray-brown foamy solid was slurried with 20ml of acetonitrile for 1 hour, and suction filtered to obtain 1.14g of off-white solid, which was the impurity EP-ZG, with a yield of 37.70% and a purity of 95%.

Embodiment 2

[0021]

[0022] Take a 500mL three-necked flask, add 1.2g of budesonide and 240mL of isopropanol, stir to dissolve; then add 0.24g of triphenylphosphine rhodium chloride, the system changes from colorless and clear to reddish brown, and hydrogen gas is introduced into the solution to replace Three times, the reaction was carried out at room temperature until the liquid phase detection showed that there was no residue of the raw material budesonide; then the system was directly filtered, the filtrate was concentrated and dried to obtain a black oil, and the black oil was separated by mixing column chromatography to obtain 1.02 g of gray-brown foam The obtained gray-brown foamy solid was slurried with 10 ml of acetonitrile for 1 h, and suction-filtered to obtain 0.47 g of impurity EP-ZG, with a yield of 39.10% and a purity of 93.7%.

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Abstract

The invention provides a synthesis method of a budesonide impurity EP-ZG. The synthesis method comprises the steps that budesonide serves as a raw material and is dissolved in an organic solvent, andthen a metal catalyst is added, so that the budesonide and hydrogen are subjected to a reduction reaction to generate the impurity EP-ZG. The synthesis method is simple in process route, convenient tooperate, good in selectivity and high in yield; the synthesized budesonide impurity EP-ZG can serve as a reference substance for detecting and studying the budesonide and be applied to quality control over the budesonide and preparations related to the budesonide to control the purity of budesonide active pharmaceutical ingredients or preparations thereof.

Description

technical field [0001] The invention belongs to the field of drug impurity synthesis, in particular to a method for synthesizing budesonide impurity EP-ZG. Background technique [0002] Budesonide is a glucocorticoid asthma treatment drug, which belongs to the adrenal cortex hormone drugs. It was first developed and marketed by AstraZeneca Pharmaceutical Company in 1981. It has a strong local anti-inflammatory effect, can inhibit early bronchospasm and late allergic reaction, and is one of the important drugs for the treatment of allergic asthma. Among similar drugs, budesonide has highly effective local anti-inflammatory effect, long-lasting effect and no systemic adrenal cortex hormone effect, so it is more suitable for local administration. [0003] At present, budesonide is mainly used in the treatment of asthma and allergic rhinitis in two different dosage forms, aerosol and suspension respectively. The dosage forms with budesonide as the active ingredient on the mark...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J71/00
CPCC07J71/0031
Inventor 李久青蔡报彬浮绍东李昊蔡保理
Owner BIONNA (BEIJING) MEDICAL TECH CO LTD